UniProt	IUPHAR	Receptor family	Cl.	Species	Method	PDB	Refined structure	Resolution	Preferred chain	State	Degree active (%)	% of Seq	Family	Subtype	Note	% of Seq	Fusion	Antibodies	Name	Type	Function	Name	Type	D2x50 S3x39	Sodium in structure	Authors	Reference	PDB Date

OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	1F88	1F88_refined	2.8	A	Inactive	22	97	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M	10.1126/SCIENCE.289.5480.739	2000-08-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	1HZX	-	2.8	A	Inactive	22	98	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Teller DC, Okada T, Behnke CA, Palczewski K, Stenkamp RE	10.1021/BI0155091	2001-07-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	1L9H	-	2.6	A	Inactive	22	98	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Okada T, Fujiyoshi Y, Silow M, Navarro J, Landau EM, Shichida Y	10.1073/PNAS.082666399	2002-05-15	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	1GZM	1GZM_refined	2.7	A	Inactive	22	94	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	-	10.1016/J.JMB.2004.08.090	2003-11-20	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	1U19	1U19_refined	2.2	A	Inactive	22	100	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Okada T, Sugihara M, Bondar AN, Elstner M, Entel P, Buss V	10.1016/J.JMB.2004.07.044	2004-10-12	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2HPY	-	2.8	B	Inactive	22	100	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Nakamichi H, Okada T	10.1073/PNAS.0601765103	2006-08-22	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2G87	-	2.6	A	Inactive	22	100	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Nakamichi H, Okada T	10.1002/ANIE.200600595	2006-09-02	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2I35	-	3.8	A	Inactive	22	94	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K	10.1073/PNAS.0608022103	2006-10-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2I36	-	4.1	A	Inactive	22	94	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K	10.1073/PNAS.0608022103	2006-10-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2I37	-	4.2	A	Inactive	22	91	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Salom D, Lodowski DT, Stenkamp RE, Le Trong I, Golczak M, Jastrzebska B, Harris T, Ballesteros JA, Palczewski K	10.1073/PNAS.0608022103	2006-10-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2J4Y	-	3.4	B	Inactive	22	94	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Standfuss J, Xie G, Edwards PC, Burghammer M, Oprian DD, Schertler GF	10.1016/J.JMB.2007.03.007	2007-09-25	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2PED	-	3.0	B	Inactive	22	100	-	-	-	-	-	-	Retinal (9-cis)	small-molecule	Inverse agonist	-	-	No	No	Nakamichi H, Buss V, Okada T	10.1529/BIOPHYSJ.107.108225	2007-10-30	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	2RH1	-	2.4	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC	10.1126/SCIENCE.1150577	2007-10-30	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	2R4R	-	3.4	A	Inactive	1	52	-	-	-	-	-	Antibody	-	-	-	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK	10.1038/NATURE06325	2007-11-06	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	2R4S	-	3.4	A	Inactive	1	52	-	-	-	-	-	Antibody	-	-	-	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK	10.1038/NATURE06325	2007-11-06	Yes
OPSD	Rhodopsin	Opsins	A	Japanese flying squid	X-ray	2ZIY	-	3.7	A	Inactive	16	83	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	Yes	No	Shimamura T, Hiraki K, Takahashi N, Hori T, Ago H, Masuda K, Takio K, Ishiguro M, Miyano M	10.1074/JBC.C800040200	2008-05-06	Yes
OPSD	Rhodopsin	Opsins	A	Japanese flying squid	X-ray	2Z73	2Z73_refined	2.5	A	Inactive	16	78	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	Yes	No	Murakami M, Kouyama T	10.1038/NATURE06925	2008-05-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3D4S	3D4S_refined	2.8	A	Inactive	0	67	-	-	-	-	T4-Lysozyme	-	timolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Hanson MA, Cherezov V, Griffith MT, Roth CB, Jaakola VP, Chien EY, Velasquez J, Kuhn P, Stevens RC	10.1016/J.STR.2008.05.001	2008-06-17	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2VT4	-	2.7	B	Inactive	0	57	-	-	-	-	-	-	(S)-Cyanopindolol	small-molecule	Antagonist	-	-	Yes	No	Warne T, Serrano-Vega MJ, Baker JG, Moukhametzianov R, Edwards PC, Henderson R, Leslie AG, Tate CG, Schertler GF	10.1038/NATURE07101	2008-06-24	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3CAP	-	2.9	A	Active	97	94	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Park JH, Scheerer P, Hofmann KP, Choe HW, Ernst OP	10.1038/NATURE07063	2008-06-24	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3C9L	3C9L_refined	2.7	A	Inactive	22	94	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Stenkamp RE	10.1107/S0907444908017162	2008-08-05	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3C9M	-	3.4	A	Inactive	22	94	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Stenkamp RE	10.1107/S0907444908017162	2008-08-05	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3DQB	3DQB_refined	3.2	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP	10.1038/NATURE07330	2008-09-23	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3EML	-	2.6	A	Inactive	1	70	-	-	-	-	T4-Lysozyme	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, Ijzerman AP, Stevens RC	10.1126/SCIENCE.1164772	2008-10-14	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3KJ6	-	3.4	A	Inactive	1	54	-	-	-	-	-	Antibody	-	-	-	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Bokoch MP, Zou Y, Rasmussen SG, Liu CW, Nygaard R, Rosenbaum DM, Fung JJ, Choi HJ, Thian FS, Kobilka TS, Puglisi JD, Weis WI, Pardo L, Prosser RS, Mueller L, Kobilka BK	10.1038/NATURE08650	2010-02-16	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3NY8	3NY8_refined	2.8	A	Inactive	0	67	-	-	-	-	T4-Lysozyme	-	CHEMBL1233766	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Wacker D, Fenalti G, Brown MA, Katritch V, Abagyan R, Cherezov V, Stevens RC	10.1021/JA105108Q	2010-08-11	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3NY9	3NY9_refined	2.8	A	Inactive	0	67	-	-	-	-	T4-Lysozyme	-	CHEMBL1233771	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Wacker D, Fenalti G, Brown MA, Katritch V, Abagyan R, Cherezov V, Stevens RC	10.1021/JA105108Q	2010-08-11	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3NYA	3NYA_refined	3.2	A	Inactive	0	67	-	-	-	-	T4-Lysozyme	-	CHEMBL1160734	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Wacker D, Fenalti G, Brown MA, Katritch V, Abagyan R, Cherezov V, Stevens RC	10.1021/JA105108Q	2010-08-11	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	3ODU	3ODU_refined	2.5	A	Inactive	3	83	-	-	-	-	T4-Lysozyme	-	isothiourea-1t	small-molecule	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC	10.1126/SCIENCE.1194396	2010-10-27	Yes
DRD3	D₃	Dopamine	A	Human	X-ray	3PBL	3PBL_refined	2.9	A	Inactive	1	68	-	-	-	-	T4-Lysozyme	-	eticlopride	small-molecule	Antagonist	dopamine	small-molecule	Yes	No	Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC	10.1126/SCIENCE.1197410	2010-11-03	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3PDS	3PDS_refined	3.5	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	FAUC50	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, Rasmussen SG, Choi HJ, Devree BT, Sunahara RK, Chae PS, Gellman SH, Dror RO, Shaw DE, Weis WI, Caffrey M, Gmeiner P, Kobilka BK	10.1038/NATURE09665	2011-01-12	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3PXO	-	3.0	A	Active	97	94	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP	10.1038/NATURE09789	2011-03-09	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	2X72	2X72_refined	3.0	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Standfuss J, Edwards PC, D'Antona A, Fransen M, Xie G, Oprian DD, Schertler GF	10.1038/NATURE09795	2011-03-16	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	2YDV	2YDV_refined	2.6	A	Active	74	75	-	-	-	-	-	-	NECA	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG	10.1038/NATURE10136	2011-05-18	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2YCY	-	3.2	A	Inactive	0	60	-	-	-	-	-	-	(S)-Cyanopindolol	small-molecule	Antagonist	-	-	Yes	No	Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF	10.1073/PNAS.1100185108	2011-06-08	Yes
OPSD	Rhodopsin	Opsins	A	Japanese flying squid	X-ray	3AYN	-	2.7	B	Inactive	16	77	-	-	-	-	-	-	Retinal (9-cis)	small-molecule	Inverse agonist	-	-	Yes	No	Murakami M, Kouyama T	10.1016/J.JMB.2011.08.044	2011-08-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3RFM	3RFM_refined	3.6	A	Inactive	1	71	-	-	-	-	-	-	caffeine	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH	10.1016/J.STR.2011.06.014	2011-09-07	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3VGA	-	3.1	A	Inactive	1	72	-	-	-	-	-	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Hino T, Arakawa T, Iwanari H, Yurugi-Kobayashi T, Ikeda-Suno C, Nakada-Nakura Y, Kusano-Arai O, Weyand S, Shimamura T, Nomura N, Cameron AD, Kobayashi T, Hamakubo T, Iwata S, Murata T	10.1038/NATURE10750	2012-02-01	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3UZA	3UZA_refined	3.3	A	Inactive	1	71	-	-	-	-	-	-	compound 4g [PMID: 22220592]	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH.	10.1021/jm201376w	2012-03-21	Yes
OPRM	μ	Opioid	A	Mouse	X-ray	4DKL	4DKL_refined	2.8	A	Inactive	3	71	-	-	-	-	T4-Lysozyme	-	Methyl 4-[[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-4-oxobutanoate	small-molecule	Antagonist	-	-	Yes	No	Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S	10.1038/NATURE10954	2012-03-21	Yes
OPRD	δ	Opioid	A	Mouse	X-ray	4EJ4	4EJ4_refined	3.4	A	Inactive	3	76	-	-	-	-	T4-Lysozyme	-	naltrindole	small-molecule	Antagonist	α-neoendorphin, [Leu]enkephalin, [Met]enkephalin	peptide	Yes	No	Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK	10.1038/NATURE11111	2012-05-16	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4GRV	4GRV_refined	2.8	A	Active	92	69	-	-	-	-	T4-Lysozyme	-	JMV431	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	White JF, Noinaj N, Shibata Y, Love J, Kloss B, Xu F, Gvozdenovic-Jeremic J, Shah P, Shiloach J, Tate CG, Grisshammer R	10.1038/NATURE11558	2012-10-17	Yes
5HT1B	5-HT_1B	5-Hydroxytryptamine	A	Human	X-ray	4IAQ	4IAQ_refined	2.8	A	Inactive	14	70	-	-	-	-	BRIL	-	dihydroergotamine	small-molecule	Agonist	tryptamine, 5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE	10.1126/SCIENCE.1232807	2013-03-13	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	3ZPR	3ZPR_refined	2.7	B	Inactive	0	61	-	-	-	-	-	-	CHEMBL1559535	small-molecule	Antagonist	-	-	Yes	Yes	Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M.	10.1021/jm400140q	2013-04-03	Yes
GLR	glucagon	Glucagon	B1	Human	X-ray	4L6R	4L6R_refined	3.3	A	Inactive	5	61	-	-	-	-	BRIL	-	-	-	-	glucagon	peptide	No	No	Siu FY, He M, de Graaf C, Han GW, Yang D, Zhang Z, Zhou C, Xu Q, Wacker D, Joseph JS, Liu W, Lau J, Cherezov V, Katritch V, Wang MW, Stevens RC	10.1038/nature12393	2013-07-24	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	4LDE	4LDE_refined	2.8	A	Active	100	69	-	-	-	-	T4-Lysozyme	Nanobody	CHEMBL1615159	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK	10.1038/NATURE12572	2013-09-25	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	4MQS	4MQS_refined	3.5	A	Active	99	59	-	-	-	-	-	Nanobody	iperoxo	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK	10.1038/NATURE12735	2013-11-27	Yes
SMO	SMO	Frizzled	F	Human	X-ray	4N4W	4N4W_refined	2.8	A	Inactive	0	44	-	-	-	-	BRIL	-	SANT-1	small-molecule	Antagonist	-	-	No	No	Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC	10.1038/NCOMMS5355	2014-01-22	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4BWB	-	3.6	A	Inactive	2	72	-	-	-	-	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A	10.1073/PNAS.1317903111	2014-01-29	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	4BVN	4BVN_refined	2.1	A	Inactive	0	60	-	-	-	-	-	-	(S)-Cyanopindolol	small-molecule	Antagonist	-	-	Yes	Yes	Miller-Gallacher JL, Nehme R, Warne T, Edwards PC, Schertler GF, Leslie AG, Tate CG	10.1371/JOURNAL.PONE.0092727	2014-04-02	Yes
P2Y12	P2Y₁₂	P2Y	A	Human	X-ray	4PY0	4PY0_refined	3.1	A	Intermediate	42	83	-	-	-	-	BRIL	-	2MeSATP	small-molecule	Agonist (partial)	ATP, ADP	small-molecule	Yes	No	Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q	10.1038/NATURE13288	2014-04-30	Yes
SMO	SMO	Frizzled	F	Human	X-ray	4QIN	4QIN_refined	2.6	A	Inactive	11	43	-	-	-	-	BRIL	-	SAG1.5	small-molecule	Agonist	-	-	No	No	Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC	10.1038/NCOMMS5355	2014-07-23	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Rat	X-ray	4U16	4U16_refined	3.7	B	Inactive	3	47	-	-	-	-	T4-Lysozyme	-	N-methyl scopolamine	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Thorsen TS, Matt R, Weis WI, Kobilka BK	10.1016/J.STR.2014.08.022	2014-11-26	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	4RWS	4RWS_refined	3.1	A	Inactive	3	78	-	-	-	-	T4-Lysozyme	-	viral macrophage inflammatory protein-II	peptide	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Qin L, Kufareva I, Holden LG, Wang C, Zheng Y, Zhao C, Fenalti G, Wu H, Han GW, Cherezov V, Abagyan R, Stevens RC, Handel TM	10.1126/SCIENCE.1261064	2015-02-11	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	X-ray	4Z34	4Z34_refined	3.0	A	Inactive	1	80	-	-	-	-	BRIL	-	ONO-9780307	small-molecule	Antagonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA	10.1016/J.CELL.2015.06.002	2015-06-03	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4XEE	4XEE_refined	2.9	A	Active	92	71	-	-	-	-	T4-Lysozyme	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Krumm BE, White JF, Shah P, Grisshammer R	10.1038/NCOMMS8895	2015-07-29	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	5CGC	5CGC_refined	3.1	A	Inactive	-	20	-	-	-	-	T4-Lysozyme	-	CHEMBL3603915	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M.	10.1021/acs.jmedchem.5b00892	2015-08-12	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	4ZUD	4ZUD_refined	2.8	A	Inactive	3	75	-	-	-	-	BRIL	-	OLMESARTAN	small-molecule	Inverse agonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC	10.1074/JBC.M115.689000	2015-10-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4X1H	4X1H_refined	2.3	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	B-Nonylglucoside	small-molecule	unknown	-	-	No	No	Blankenship E, Vahedi-Faridi A, Lodowski DT	10.1016/J.STR.2015.09.015	2015-11-04	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	5D5B	5D5B_refined	3.8	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M	10.1107/S2059798315021683	2016-01-13	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	X-ray	5DSG	5DSG_refined	2.6	B	Inactive	3	60	-	-	-	-	T4-Lysozyme	-	tiotropium	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A	10.1038/NATURE17188	2016-03-16	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5IU4	5IU4_refined	1.7	A	Inactive	1	71	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.	10.1021/acs.jmedchem.6b00653	2016-06-29	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5IU7	5IU7_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	2-(Furan-2-yl)-5-N-[2-(4-phenylpiperidin-1-yl)ethyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.	10.1021/acs.jmedchem.6b00653	2016-06-29	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5IUB	5IUB_refined	2.1	A	Inactive	1	71	-	-	-	-	BRIL	-	CHEMBL184061	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.	10.1021/acs.jmedchem.6b00653	2016-06-29	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5G53	5G53_refined	3.4	A	Active	100	68	Gs	αs	Engineered G protein	50	-	-	NECA	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG	10.1038/NATURE18966	2016-08-03	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	5GLI	5GLI_refined	2.5	A	Inactive	5	71	-	-	-	-	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T	10.1038/nature19319	2016-09-07	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5K2C	5K2C_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V	10.1126/SCIADV.1600292	2016-09-21	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	5U09	5U09_refined	2.6	A	Inactive	9	60	-	-	-	-	Glycogen synthase	-	taranabant	small-molecule	Inverse agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J, Rosenbaum DM	10.1038/NATURE20613	2016-12-07	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5UIG	5UIG_refined	3.5	A	Inactive	19	70	-	-	-	-	BRIL	-	5-Amino-N-[(2-Methoxyphenyl)methyl]-2-(3-Methylphenyl)-2h-1,2,3-Triazole-4-Carboximidamide	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Sun B, Bachhawat P, Chu ML, Wood M, Ceska T, Sands ZA, Mercier J, Lebon F, Kobilka TS, Kobilka BK	10.1073/PNAS.1621423114	2017-02-08	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	5UNF	5UNF_refined	2.8	A	Active	99	79	-	-	-	-	BRIL	-	compound 1 [PMID: 28379944]	small-molecule	Antagonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V	10.1038/NATURE22035	2017-04-05	Yes
PAR2	PAR2	Proteinase-activated	A	Human	X-ray	5NDZ	5NDZ_refined	3.6	A	Intermediate	42	74	-	-	-	-	BRIL	-	AZ3451	small-molecule	Allosteric antagonist	-	-	Yes	Yes	Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N	10.1038/NATURE22309	2017-05-03	Yes
SMO	SMO	Frizzled	F	Human	X-ray	5V56	5V56_refined	2.9	B	Inactive	1	61	-	-	-	-	Flavodoxin	-	N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide	small-molecule	Antagonist	-	-	No	No	Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F	10.1038/NCOMMS15383	2017-05-24	Yes
GLR	glucagon	Glucagon	B1	Human	X-ray	5XEZ	5XEZ_refined	3.0	B	Inactive	0	82	-	-	-	-	T4-Lysozyme	Antibody	NNC0640	small-molecule	NAM	glucagon	peptide	No	No	Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B	10.1038/NATURE22363	2017-05-24	Yes
FFAR1	FFA1	Free fatty acid	A	Human	X-ray	5TZR	5TZR_refined	2.2	A	Intermediate	42	91	-	-	-	-	T4-Lysozyme	-	MK-8666	small-molecule	Agonist	docosahexaenoic acid, oleic acid, α-linolenic acid, myristic acid	small-molecule	No	No	Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM	10.1038/NSMB.3417	2017-06-07	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	5XR8	5XR8_refined	3.0	A	Active	96	60	-	-	-	-	Flavodoxin	-	AM841	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ	10.1038/NATURE23272	2017-07-12	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5MZP	5MZP_refined	2.1	A	Inactive	1	71	-	-	-	-	BRIL	-	caffeine	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM	10.1016/j.str.2017.06.012	2017-07-26	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	5TUD	5TUD_refined	3.0	D	Active	87	58	-	-	-	-	BRIL	Antibody	ergotamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Ishchenko A, Wacker D, Kapoor M, Zhang A, Han GW, Basu S, Patel N, Messerschmidt M, Weierstall U, Liu W, Katritch V, Roth BL, Stevens RC, Cherezov V	10.1073/PNAS.1700891114	2017-07-26	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	5XPR	5XPR_refined	3.6	A	Inactive	5	69	-	-	-	-	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O	10.1038/NSMB.3450	2017-08-16	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5NM4	-	1.7	A	Inactive	1	73	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J	10.1038/S41467-017-00630-4	2017-09-27	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	5WQC	5WQC_refined	2.0	A	Inactive	1	68	-	-	-	-	Glycogen synthase	-	EMPA	small-molecule	Antagonist	orexin-A, orexin-B	peptide	Yes	No	Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T	10.1016/J.STR.2017.11.005	2017-11-29	Yes
Q9WTK1	BLT₁	Leukotriene	A	Guinea pig	X-ray	5X33	5X33_refined	3.7	A	Inactive	3	78	-	-	-	-	T4-Lysozyme	-	BIIL 260	small-molecule	Antagonist	-	-	Yes	No	Hori T, Okuno T, Hirata K, Yamashita K, Kawano Y, Yamamoto M, Hato M, Nakamura M, Shimizu T, Yokomizo T, Miyano M, Yokoyama S	10.1038/NCHEMBIO.2547	2018-01-03	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OLH	5OLH_refined	2.6	A	Inactive	1	72	-	-	-	-	BRIL	-	vipadenant	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OM1	5OM1_refined	2.1	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL2024114	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
5HT1B	5-HT_1B	5-Hydroxytryptamine	A	Human	X-ray	5V54	5V54_refined	3.9	A	Inactive	14	71	-	-	-	-	BRIL	-	CHEMBL428892	small-molecule	Antagonist	tryptamine, 5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2018-02-07	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5WF6	5WF6_refined	2.9	A	Active	74	68	-	-	-	-	T4-Lysozyme	-	UK-432,097	small-molecule	Agonist	adenosine	small-molecule	No	No	-	-	2018-02-21	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	6FFI	6FFI_refined	2.2	A	Inactive	-	20	-	-	-	-	T4-Lysozyme	-	methoxy-MPEP	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM	10.1021/ACS.JMEDCHEM.7B01722	2018-03-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FK7	6FK7_refined	2.6	A	Active	97	94	-	-	-	-	-	-	(2~{S})-2-(4-chlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FKA	6FKA_refined	2.7	A	Active	97	94	-	-	-	-	-	-	(2~{S})-2-(3,4-dichlorophenyl)-3-methyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
NPY1R	Y₁	Neuropeptide Y	A	Human	X-ray	5ZBH	5ZBH_refined	3.0	A	Inactive	1	78	-	-	-	-	T4-Lysozyme	-	BMS-193885	small-molecule	Antagonist	pancreatic polypeptide, neuropeptide Y, peptide YY	peptide	Yes	No	Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B	10.1038/S41586-018-0046-X	2018-04-25	Yes
Q98SW5	SMO	Frizzled	F	African clawed frog	X-ray	6D32	6D32_refined	3.8	A	Active	78	58	-	-	-	-	BRIL	-	cyclopamine	small-molecule	Agonist (partial)	-	-	No	No	Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A	10.1016/J.CELL.2018.04.029	2018-05-23	Yes
Q80KM9	US28	Unclassified	A	strain AD169	X-ray	5WB1	5WB1_refined	3.5	A	Active	99	82	-	-	-	-	-	Nanobody	-	-	-	-	-	Yes	No	Miles TF, Spiess K, Jude KM, Tsutsumi N, Burg JS, Ingram JR, Waghray D, Hjorto GM, Larsen O, Ploegh HL, Rosenkilde MM, Garcia KC	10.7554/ELIFE.35850	2018-06-13	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	6DDE	6DDE_refined	3.5	R	Active	100	71	Gi/o	αi1	-	61	-	Antibody	DAMGO	peptide	Agonist	-	-	Yes	No	Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK	10.1038/S41586-018-0219-7	2018-06-13	Yes
AA1R	A₁	Adenosine	A	Human	cryo-EM	6D9H	6D9H_refined	3.6	R	Active	100	88	Gi/o	αi2	-	59	-	-	adenosine	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A	10.1038/S41586-018-0236-6	2018-06-20	Yes
FZD4	FZD₄	Frizzled	F	Human	X-ray	6BD4	6BD4_refined	2.4	A	Inactive	22	61	-	-	-	-	Rubredoxin	-	-	-	-	-	-	No	No	Yang S, Wu Y, Xu TH, de Waal PW, He Y, Pu M, Chen Y, DeBruine ZJ, Zhang B, Zaidi SA, Popov P, Guo Y, Han GW, Lu Y, Suino-Powell K, Dong S, Harikumar KG, Miller LJ, Katritch V, Xu HE, Shui W, Stevens RC, Melcher K, Zhao S, Xu F	10.1038/S41586-018-0447-X	2018-08-22	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	6DS0	6DS0_refined	3.2	A	Intermediate	42	59	-	-	-	-	BRIL	-	LY266097	small-molecule	Antagonist	5-hydroxytryptamine	small-molecule	Yes	No	McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL	10.1038/s41594-018-0116-7	2018-08-29	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FUF	6FUF_refined	3.1	A	Active	100	91	Gi/o	αo	Mini-Go	51	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX	10.1126/SCIADV.AAT7052	2018-10-03	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6H7M	6H7M_refined	2.8	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb6B9	levosalbutamol	small-molecule	Agonist	-	-	Yes	No	Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG	10.1126/SCIENCE.AAU5595	2018-10-17	Yes
CCR5	CCR5	Chemokine	A	Human	X-ray	6AKX	6AKX_refined	2.8	B	Inactive	16	82	-	-	-	-	Rubredoxin	-	N-[(1S)-3-{(3-exo)-3-[3-methyl-5-(propan-2-yl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}-1-(thiophen-2-yl)propyl]cyclopentanecarboxamide	small-molecule	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H.	10.1021/acs.jmedchem.8b01077	2018-10-24	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	5ZK3	5ZK3_refined	2.6	A	Inactive	3	59	-	-	-	-	BRIL	-	CHEMBL558910	small-molecule	Antagonist	acetylcholine	small-molecule	No	No	Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T	10.1038/S41589-018-0152-Y	2018-11-21	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	X-ray	6FJ3	-	2.5	A	Inactive	0	62	-	-	-	-	GlgA glycogen synthase	-	ePTH	peptide	Agonist (partial)	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Ehrenmann J, Schoppe J, Klenk C, Rappas M, Kummer L, Dore AS, Pluckthun A	10.1038/S41594-018-0151-4	2018-11-21	Yes
PE2R3	EP₃	Prostanoid	A	Human	X-ray	6M9T	6M9T_refined	2.5	A	Active	92	70	-	-	-	-	T4-Lysozyme	-	Misoprostol-FA	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Audet M, White KL, Breton B, Zarzycka B, Han GW, Lu Y, Gati C, Batyuk A, Popov P, Velasquez J, Manahan D, Hu H, Weierstall U, Liu W, Shui W, Katritch V, Cherezov V, Hanson MA, Stevens RC	10.1038/S41589-018-0160-Y	2018-12-05	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	6MET	6MET_refined	4.5	B	Inactive	16	89	-	-	-	-	-	T-cell surface glycoprotein CD4	Envelope glycoprotein gp160	protein	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B	10.1038/S41586-018-0804-9	2018-12-12	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	X-ray	6WJC	-	2.6	A	Inactive	3	62	-	-	-	-	T4-Lysozyme	-	ENDO-ATROPINE muscarinic toxin 7	small-molecule peptide	Antagonist NAM	acetylcholine	small-molecule	No	No	Maeda S, Xu J, N Kadji FM, Clark MJ, Zhao J, Tsutsumi N, Aoki J, Sunahara RK, Inoue A, Garcia KC, Kobilka BK	10.1126/SCIENCE.AAX2517	2020-07-08	Yes
ADRB2	β₂	Adrenoceptors	A	Human	cryo-EM	7BZ2	7BZ2_refined	3.8	R	Active	100	69	Gs	αs	-	50	-	Nanobody-35	arformoterol	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C	10.1038/S41421-020-0176-9	2020-08-05	Yes
GLR	glucagon	Glucagon	B1	Human	cryo-EM	6WPW	6WPW_refined	3.1	R	Active	100	83	Gs	αs	-	56	-	Nanobody-35	Glucagon derivative ZP3780	peptide	Agonist	glucagon	peptide	No	No	Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK	10.1126/SCIENCE.ABA3373	2020-08-12	Yes
VIPR1	VPAC₁	VIP and PACAP	B1	Human	cryo-EM	6VN7	6VN7_refined	3.2	R	Active	100	58	Gs	αs	-	61	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, secretin, GHRH, PACAP-38, VIP, PHI	peptide	No	No	Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y	10.1038/S41467-020-17933-8	2020-09-02	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6X18	6X18_refined	2.1	R	Active	100	83	Gs	αs	-	90	-	Nanobody-35	CHEMBL410972	protein	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Singh N, Singh D, Bhide A, Sharma R, Bhowmick S, Patel V, Modi D	10.1101/2020.08.16.252585	2020-09-09	Yes
SUCR1	succinate	Succinate	A	Rat	X-ray	6Z10	6Z10_refined	2.3	A	Intermediate	42	90	-	-	-	-	-	Nanobody-6	CHEMBL4751488	small-molecule	Antagonist	-	-	Yes	No	Velcicky J,Wilcken R,Cotesta S,Janser P,Schlapbach A,Wagner T,Piechon P,Villard F,Bouhelal R,Piller F,Harlfinger S,Stringer R,Fehlmann D,Kaupmann K,Littlewood-Evans A,Haffke M,Gommermann N	10.1021/acs.jmedchem.0c01020	2020-09-16	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	6WGT	6WGT_refined	3.4	B	Inactive	1	59	-	-	-	-	BRIL	-	Lysergide	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	Yes	No	Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL	10.1016/J.CELL.2020.08.024	2020-09-23	Yes
SMO	SMO	Frizzled	F	Human	cryo-EM	6XBJ	6XBJ_refined	3.9	R	Active	100	59	Gi/o	αi1	-	61	-	scFv16	Cholesterol	small-molecule	Agonist	-	-	No	No	Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X	10.1038/S41589-020-0646-2	2020-09-30	Yes
SMO	SMO	Frizzled	F	Human	cryo-EM	6XBM	6XBM_refined	3.2	R	Active	100	42	Gi/o	αi1	-	61	-	scFv16	24,25-Epoxy-cholesterol 24,25-Epoxy-cholesterol	small-molecule small-molecule	Agonist PAM	-	-	No	No	Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X	10.1038/S41589-020-0646-2	2020-09-30	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	3OE0	-	2.9	A	Inactive	3	78	-	-	-	-	T4-Lysozyme	-	CVX15	peptide	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC	10.1126/SCIENCE.1194396	2010-10-27	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2Y00	2Y00_refined	2.5	B	Inactive	0	62	-	-	-	-	-	-	Dobutamine	small-molecule	Agonist (partial)	-	-	Yes	No	Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG	10.1038/NATURE09746	2011-01-12	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2Y02	2Y02_refined	2.6	B	Inactive	0	62	-	-	-	-	-	-	CARMOTEROL	small-molecule	Agonist	-	-	Yes	No	Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG	10.1038/NATURE09746	2011-01-12	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3OAX	-	2.6	A	Inactive	22	100	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	No	No	Makino CL, Riley CK, Looney J, Crouch RK, Okada T	10.1016/J.BPJ.2010.08.003	2011-01-19	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2Y01	-	2.6	A	Inactive	0	59	-	-	-	-	-	-	Dobutamine	small-molecule	Agonist (partial)	-	-	Yes	No	Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG	10.1038/NATURE09746	2011-03-30	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2YCW	2YCW_refined	3.0	A	Inactive	0	61	-	-	-	-	-	-	Carazolol	small-molecule	Antagonist	-	-	Yes	No	-	-	2011-06-01	Yes
OPSD	Rhodopsin	Opsins	A	Japanese flying squid	X-ray	3AYM	-	2.8	B	Inactive	16	77	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	Yes	No	Murakami M, Kouyama T	10.1016/J.JMB.2011.08.044	2011-08-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3REY	3REY_refined	3.3	A	Inactive	1	71	-	-	-	-	-	-	xanthine amine congener	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH	10.1016/J.STR.2011.06.014	2011-09-07	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	3UON	3UON_refined	3.0	A	Inactive	3	60	-	-	-	-	T4-Lysozyme	-	CHEMBL558910	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Haga K, Kruse AC, Asada H, Yurugi-Kobayashi T, Shiroishi M, Zhang C, Weis WI, Okada T, Kobilka BK, Haga T, Kobayashi T	10.1038/NATURE10753	2012-02-01	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	X-ray	3V2Y	3V2Y_refined	2.8	A	Inactive	1	76	-	-	-	-	T4-Lysozyme	-	W146	small-molecule	Antagonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC	10.1126/SCIENCE.1215904	2012-02-15	Yes
OPRK	κ	Opioid	A	Human	X-ray	4DJH	4DJH_refined	2.9	A	Inactive	3	76	-	-	-	-	T4-Lysozyme	-	JDTic	small-molecule	Antagonist	big dynorphin, β-neoendorphin, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC	10.1038/NATURE10939	2012-03-21	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	4AMJ	4AMJ_refined	2.3	B	Inactive	0	62	-	-	-	-	-	-	CHEMBL3799125	small-molecule	Inverse agonist	-	-	Yes	No	Warne T, Edwards PC, Leslie AG, Tate CG	10.1016/J.STR.2012.03.014	2012-05-23	Yes
PAR1	PAR1	Proteinase-activated	A	Human	X-ray	3VW7	3VW7_refined	2.2	A	Intermediate	42	66	-	-	-	-	T4-Lysozyme	-	vorapaxar	small-molecule	Antagonist	thrombin	peptide	Yes	No	Zhang C, Srinivasan Y, Arlow DH, Fung JJ, Palmer D, Zheng Y, Green HF, Pandey A, Dror RO, Shaw DE, Weis WI, Coughlin SR, Kobilka BK	10.1038/NATURE11701	2012-12-12	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	3ZPQ	3ZPQ_refined	2.8	B	Inactive	0	62	-	-	-	-	-	-	CHEMBL200234	small-molecule	Antagonist	-	-	Yes	Yes	Christopher JA, Brown J, Doré AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M.	10.1021/jm400140q	2013-04-03	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4BEY	4BEY_refined	2.9	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J	10.1038/EMBOR.2013.44	2013-05-08	Yes
CCR5	CCR5	Chemokine	A	Human	X-ray	4MBS	4MBS_refined	2.7	A	Inactive	16	83	-	-	-	-	Rubredoxin	-	maraviroc	small-molecule	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Tan Q, Zhu Y, Li J, Chen Z, Han GW, Kufareva I, Li T, Ma L, Fenalti G, Li J, Zhang W, Xie X, Yang H, Jiang H, Cherezov V, Liu H, Stevens RC, Zhao Q, Wu B	10.1126/SCIENCE.1241475	2013-09-11	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	4LDO	4LDO_refined	3.2	A	Active	100	69	-	-	-	-	T4-Lysozyme	Nanobody	(-)-adrenaline	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK	10.1038/NATURE12572	2013-09-25	Yes
OPRD	δ	Opioid	A	Human	X-ray	4N6H	4N6H_refined	1.8	A	Inactive	3	81	-	-	-	-	BRIL	-	naltrindole	small-molecule	Antagonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	Yes	Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC	10.1038/NATURE12944	2013-12-25	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4BV0	-	3.1	A	Inactive	2	70	-	-	-	-	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A	10.1073/PNAS.1317903111	2014-01-29	Yes
P2Y12	P2Y₁₂	P2Y	A	Human	X-ray	4NTJ	4NTJ_refined	2.6	A	Intermediate	42	78	-	-	-	-	BRIL	-	AZD1283	small-molecule	Antagonist	ATP, ADP	small-molecule	Yes	No	Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q	10.1038/NATURE13083	2014-03-26	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	4OO9	4OO9_refined	2.6	A	Inactive	-	20	-	-	-	-	T4-Lysozyme	-	MAVOGLURANT	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Dore AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH	10.1038/NATURE13396	2014-07-02	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	4QKX	4QKX_refined	3.3	A	Active	100	69	-	-	-	-	T4-Lysozyme	Nanobody	Q27453560	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Weichert D, Kruse AC, Manglik A, Hiller C, Zhang C, Hubner H, Kobilka BK, Gmeiner P	10.1073/PNAS.1410415111	2014-07-23	Yes
OPRD	δ	Opioid	A	Human	X-ray	4RWA	4RWA_refined	3.3	A	Inactive	3	77	-	-	-	-	BRIL	-	DIPP-NH2	peptide	Antagonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V	10.1038/NSMB.2965	2015-01-14	Yes
US28	US28	Unclassified	A	strain AD169	X-ray	4XT1	-	2.9	A	Active	99	82	-	-	-	-	-	Nanobody	CX₃CL1	peptide	Agonist (partial)	-	-	Yes	No	Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC	10.1126/SCIENCE.AAA5026	2015-03-04	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	4UG2	4UG2_refined	2.6	A	Active	74	71	-	-	-	-	-	-	CGS 21680	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Lebon G, Edwards PC, Leslie AG, Tate CG	10.1124/mol.114.097360	2015-04-08	Yes
OPSD	Rhodopsin	Opsins	A	Japanese flying squid	X-ray	4WW3	4WW3_refined	2.8	A	Inactive	16	78	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	Yes	No	Murakami M, Kouyama T	10.1371/JOURNAL.PONE.0126970	2015-06-17	Yes
OPRM	μ	Opioid	A	Mouse	X-ray	5C1M	5C1M_refined	2.1	A	Active	100	74	-	-	-	-	-	Antibody	BU72	small-molecule	Agonist	-	-	Yes	No	Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK	10.1038/NATURE14886	2015-08-05	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	5A8E	5A8E_refined	2.4	A	Inactive	0	59	-	-	-	-	-	-	7-methylcyanopindolol	small-molecule	Inverse agonist	-	-	Yes	Yes	Sato T, Baker J, Warne T, Brown GA, Leslie AG, Congreve M, Tate CG	10.1124/MOL.115.101030	2015-09-30	Yes
OPRX	NOP	Opioid	A	Human	X-ray	5DHG	5DHG_refined	3.0	A	Inactive	3	76	-	-	-	-	BRIL	-	CHEMBL1783826	small-molecule	Antagonist	nociceptin/orphanin FQ	peptide	Yes	No	Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC	10.1016/J.STR.2015.07.024	2015-10-21	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	5F8U	5F8U_refined	3.4	A	Inactive	0	57	-	-	-	-	-	-	(S)-Cyanopindolol	small-molecule	Antagonist	-	-	Yes	No	Leslie AG, Warne T, Tate CG	10.1038/NSMB.3130	2015-12-23	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	4ZJC	4ZJC_refined	2.8	A	Inactive	1	72	-	-	-	-	GlgA glycogen synthase	-	SB-674042	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM	10.1038/NSMB.3183	2016-03-09	Yes
GLR	glucagon	Glucagon	B1	Human	X-ray	5EE7	5EE7_refined	2.5	A	Inactive	0	54	-	-	-	-	T4-Lysozyme	-	Octaethylene glycol monoethyl ether MK-0893	small-molecule small-molecule	Antagonist NAM	glucagon	peptide	No	No	Jazayeri A, Dore AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC, Andrews SP, Teobald I, Brown AJ, Cooke RM, Weir M, Marshall FH	10.1038/NATURE17414	2016-04-20	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5IU8	5IU8_refined	2.0	A	Inactive	1	71	-	-	-	-	BRIL	-	CHEMBL3934661	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.	10.1021/acs.jmedchem.6b00653	2016-06-29	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	5JQH	5JQH_refined	3.2	A	Inactive	0	70	-	-	-	-	T4-Lysozyme	Nanobody	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Staus DP, Strachan RT, Manglik A, Pani B, Kahsai AW, Kim TH, Wingler LM, Ahn S, Chatterjee A, Masoudi A, Kruse AC, Pardon E, Steyaert J, Weis WI, Prosser RS, Kobilka BK, Costa T, Lefkowitz RJ	10.1038/NATURE18636	2016-07-13	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	5DYS	5DYS_refined	2.3	A	Active	97	94	-	-	-	-	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J	10.15252/EMBR.201642671	2016-08-10	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	5D6L	5D6L_refined	3.2	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ma P, Weichert D, Aleksandrov LA, Jensen TJ, Riordan JR, Liu X, Kobilka BK, Caffrey M	10.1038/NPROT.2017.057	2016-08-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5K2B	5K2B_refined	2.5	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V	10.1126/SCIADV.1600292	2016-09-21	Yes
CCR9	CCR9	Chemokine	A	Human	X-ray	5LWE	-	2.8	B	Inactive	52	67	-	-	-	-	-	-	vercirnon	small-molecule	Allosteric antagonist	CCL25	peptide	No	No	Oswald C, Rappas M, Kean J, Dore AS, Errey JC, Bennett K, Deflorian F, Christopher JA, Jazayeri A, Mason JS, Congreve M, Cooke RM, Marshall FH	10.1038/NATURE20606	2016-12-07	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	5TVN	5TVN_refined	2.9	A	Intermediate	42	61	-	-	-	-	BRIL	-	Lysergide	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, Lansu K, Schools ZL, Che T, Nichols DE, Shoichet BK, Dror RO, Roth BL	10.1016/J.CELL.2016.12.033	2017-02-01	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	5TE5	5TE5_refined	4.0	A	Inactive	22	100	-	-	-	-	-	-	10,20-Methanoretinal	small-molecule	Agonist	-	-	No	No	Gulati S, Jastrzebska B, Banerjee S, Placeres AL, Miszta P, Gao S, Gunderson K, Tochtrop GP, Filipek S, Katayama K, Kiser PD, Mogi M, Stewart PL, Palczewski K	10.1073/PNAS.1617446114	2017-03-15	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	5UNG	5UNG_refined	2.8	B	Active	99	83	-	-	-	-	BRIL	-	compound 1 [PMID: 28379944]	small-molecule	Antagonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V	10.1038/NATURE22035	2017-04-05	Yes
PAR2	PAR2	Proteinase-activated	A	Human	X-ray	5NJ6	5NJ6_refined	4.0	A	Intermediate	42	74	-	-	-	-	BRIL	Fab3949	-	-	-	-	-	Yes	No	Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N	10.1038/NATURE22309	2017-05-03	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5UVI	5UVI_refined	3.2	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Martin-Garcia JM, Conrad CE, Nelson G, Stander N, Zatsepin NA, Zook J, Zhu L, Geiger J, Chun E, Kissick D, Hilgart MC, Ogata C, Ishchenko A, Nagaratnam N, Roy-Chowdhury S, Coe J, Subramanian G, Schaffer A, James D, Ketwala G, Venugopalan N, Xu S, Corcoran S, Ferguson D, Weierstall U, Spence JCH, Cherezov V, Fromme P, Fischetti RF, Liu W	10.1107/S205225251700570X	2017-05-24	Yes
SMO	SMO	Frizzled	F	Human	X-ray	5V57	5V57_refined	3.0	A	Inactive	1	62	-	-	-	-	Flavodoxin	-	N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-4-nitro-2-(trifluoromethyl)benzamide	small-molecule	Antagonist	-	-	No	No	Zhang X, Zhao F, Wu Y, Yang J, Han GW, Zhao S, Ishchenko A, Ye L, Lin X, Ding K, Dharmarajan V, Griffin PR, Gati C, Nelson G, Hunter MS, Hanson MA, Cherezov V, Stevens RC, Tan W, Tao H, Xu F	10.1038/NCOMMS15383	2017-05-24	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5JTB	5JTB_refined	2.8	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Melnikov I, Polovinkin V, Kovalev K, Gushchin I, Shevtsov M, Shevchenko V, Mishin A, Alekseev A, Rodriguez-Valera F, Borshchevskiy V, Cherezov V, Leonard GA, Gordeliy V, Popov A	10.1126/SCIADV.1602952	2017-05-31	Yes
APJ	apelin	Apelin	A	Human	X-ray	5VBL	-	2.6	B	Inactive	3	79	-	-	-	-	Rubredoxin	-	AMG3054	peptide	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Ma Y, Yue Y, Ma Y, Zhang Q, Zhou Q, Song Y, Shen Y, Li X, Ma X, Li C, Hanson MA, Han GW, Sickmier EA, Swaminath G, Zhao S, Stevens RC, Hu LA, Zhong W, Zhang M, Xu F	10.1016/J.STR.2017.04.008	2017-05-31	Yes
CCR5	CCR5	Chemokine	A	Human	X-ray	5UIW	-	2.2	A	Inactive	16	85	-	-	-	-	Rubredoxin	-	5P7-CCL5	protein	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Zheng Y, Han GW, Abagyan R, Wu B, Stevens RC, Cherezov V, Kufareva I, Handel TM	10.1016/J.IMMUNI.2017.05.002	2017-06-28	Yes
OPSD	Rhodopsin	Opsins	A	Human	X-ray	5W0P	5W0P_refined	3.0	D	Active	100	93	Visual	S-arrestin	-	90	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhou XE, He Y, de Waal PW, Gao X, Kang Y, Van Eps N, Yin Y, Pal K, Goswami D, White TA, Barty A, Latorraca NR, Chapman HN, Hubbell WL, Dror RO, Stevens RC, Cherezov V, Gurevich VV, Griffin PR, Ernst OP, Melcher K, Xu HE	10.1016/J.CELL.2017.07.002	2017-08-09	Yes
DRD4	D₄	Dopamine	A	Human	X-ray	5WIV	-	2.1	A	Inactive	1	58	-	-	-	-	BRIL	-	[3H]NEMONAPRIDE	small-molecule	Antagonist	dopamine	small-molecule	Yes	Yes	Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang XP, Dror RO, Shoichet BK, Roth BL	10.1126/SCIENCE.AAN5468	2017-10-18	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	5WS3	5WS3_refined	2.3	A	Inactive	1	70	-	-	-	-	Glycogen synthase	-	EMPA	small-molecule	Antagonist	orexin-A, orexin-B	peptide	Yes	No	Suno R, Kimura KT, Nakane T, Yamashita K, Wang J, Fujiwara T, Yamanaka Y, Im D, Horita S, Tsujimoto H, Tawaramoto MS, Hirokawa T, Nango E, Tono K, Kameshima T, Hatsui T, Joti Y, Yabashi M, Shimamoto K, Yamamoto M, Rosenbaum DM, Iwata S, Shimamura T, Kobayashi T	10.1016/J.STR.2017.11.005	2017-12-13	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6AQF	6AQF_refined	2.5	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Eddy MT, Lee MY, Gao ZG, White KL, Didenko T, Horst R, Audet M, Stanczak P, McClary KM, Han GW, Jacobson KA, Stevens RC, Wuthrich K	10.1016/J.CELL.2017.12.004	2018-01-10	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OLO	5OLO_refined	3.1	A	Inactive	1	72	-	-	-	-	BRIL	-	tozadenant	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OM4	5OM4_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL2024114	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	X-ray	6BQG	6BQG_refined	3.0	A	Active	87	62	-	-	-	-	BRIL	-	ergotamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ	10.1016/j.cell.2018.01.001	2018-02-14	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5WF5	5WF5_refined	2.6	A	Active	74	69	-	-	-	-	T4-Lysozyme	-	UK-432,097	small-molecule	Agonist	adenosine	small-molecule	No	No	White KL, Eddy MT, Gao ZG, Han GW, Lian T, Deary A, Patel N, Jacobson KA, Katritch V, Stevens RC	10.1016/J.STR.2017.12.013	2018-02-21	Yes
DRD2	D₂	Dopamine	A	Human	X-ray	6CM4	6CM4_refined	2.9	A	Inactive	1	59	-	-	-	-	T4-Lysozyme	-	risperidone	small-molecule	Inverse agonist	dopamine	small-molecule	Yes	No	Wang S, Che T, Levit A, Shoichet BK, Wacker D, Roth BL	10.1038/NATURE25758	2018-03-14	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FK8	6FK8_refined	2.9	A	Active	97	94	-	-	-	-	-	-	(2~{R},3~{S})-3-azanyl-2-(4-chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FKB	6FKB_refined	3.0	A	Active	97	94	-	-	-	-	-	-	2-(4-Chlorophenyl)-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-ethanone	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
NPY1R	Y₁	Neuropeptide Y	A	Human	X-ray	5ZBQ	5ZBQ_refined	2.7	A	Inactive	1	80	-	-	-	-	T4-Lysozyme	-	CHEMBL3747822	small-molecule	Antagonist	pancreatic polypeptide, neuropeptide Y, peptide YY	peptide	Yes	No	Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kogler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B	10.1038/S41586-018-0046-X	2018-04-25	Yes
Q98SW5	SMO	Frizzled	F	African clawed frog	X-ray	6D35	6D35_refined	3.9	A	Active	78	58	-	-	-	-	BRIL	-	Cholesterol	small-molecule	Agonist	-	-	No	No	Huang P, Zheng S, Wierbowski BM, Kim Y, Nedelcu D, Aravena L, Liu J, Kruse AC, Salic A	10.1016/J.CELL.2018.04.029	2018-05-23	Yes
C5AR1	C5a₁	Complement peptide	A	Human	X-ray	6C1R	6C1R_refined	2.2	B	Inactive	6	83	-	-	-	-	BRIL	-	PMX53 avacopan	peptide small-molecule	Antagonist NAM	C3a, C5a, C5a des-Arg, ribosomal protein S19	peptide	Yes	No	Liu H, Kim HR, Deepak RNVK, Wang L, Chung KY, Fan H, Wei Z, Zhang C	10.1038/S41594-018-0067-Z	2018-05-30	Yes
PTAFR	PAF	Platelet-activating factor	A	Human	X-ray	5ZKP	5ZKP_refined	2.8	A	Other	-	85	-	-	-	-	Flavodoxin	-	foropafant	small-molecule	Antagonist	methylcarbamyl PAF, PAF	small-molecule	Yes	No	Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B	10.1038/S41594-018-0068-Y	2018-06-20	Yes
PTAFR	PAF	Platelet-activating factor	A	Human	X-ray	5ZKQ	5ZKQ_refined	2.9	B	Intermediate	42	83	-	-	-	-	T4-Lysozyme	-	ABT-491	small-molecule	Inverse agonist	methylcarbamyl PAF, PAF	small-molecule	Yes	No	Cao C, Tan Q, Xu C, He L, Yang L, Zhou Y, Zhou Y, Qiao A, Lu M, Yi C, Han GW, Wang X, Li X, Yang H, Rao Z, Jiang H, Zhao Y, Liu J, Stevens RC, Zhao Q, Zhang XC, Wu B	10.1038/S41594-018-0068-Y	2018-06-20	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	5XJM	5XJM_refined	3.2	A	Active	100	78	-	-	-	-	BRIL	Fab	CHEMBL404594	protein	Agonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Asada H, Horita S, Hirata K, Shiroishi M, Shiimura Y, Iwanari H, Hamakubo T, Shimamura T, Nomura N, Kusano-Arai O, Uemura T, Suno C, Kobayashi T, Iwata S	10.1038/S41594-018-0079-8	2018-07-11	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	6DRX	6DRX_refined	3.1	A	Intermediate	42	59	-	-	-	-	BRIL	-	lisuride	small-molecule	Antagonist	5-hydroxytryptamine	small-molecule	Yes	No	McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL	10.1038/s41594-018-0116-7	2018-08-29	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	6E3Y	6E3Y_refined	3.3	R	Active	100	75	Gs	αs	-	48	-	Nanobody-35 RAMP1	Calcitonin gene-related peptide 1	peptide	Agonist	-	-	No	No	Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM	10.1038/S41586-018-0535-Y	2018-09-19	Yes
CCR5	CCR5	Chemokine	A	Human	X-ray	6AKY	6AKY_refined	2.8	A	Inactive	16	81	-	-	-	-	Rubredoxin	-	CCR5 antagonist 34	small-molecule	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Peng P, Chen H, Zhu Y, Wang Z, Li J, Luo RH, Wang J, Chen L, Yang LM, Jiang H, Xie X, Wu B, Zheng YT, Liu H.	10.1021/acs.jmedchem.8b01077	2018-10-24	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	5ZK8	5ZK8_refined	3.0	A	Inactive	3	59	-	-	-	-	BRIL	-	N-methyl scopolamine	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T	10.1038/S41589-018-0152-Y	2018-11-21	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	6IGK	6IGK_refined	2.0	A	Inactive	5	70	-	-	-	-	T4-Lysozyme	-	endothelin-3	peptide	Agonist	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T, Nureki O	10.1038/S41467-018-07094-0	2018-11-21	Yes
PE2R4	EP₄	Prostanoid	A	Human	X-ray	5YWY	5YWY_refined	3.2	A	Inactive	11	57	-	-	-	-	-	Fab	ONO-AE3-208	small-molecule	Antagonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	No	No	Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T	10.1038/S41589-018-0131-3	2018-12-05	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	6MEO	6MEO_refined	3.9	B	Inactive	16	89	-	-	-	-	-	T-cell surface glycoprotein CD4	Envelope glycoprotein gp160	protein	Antagonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Shaik MM, Peng H, Lu J, Rits-Volloch S, Xu C, Liao M, Chen B	10.1038/S41586-018-0804-9	2018-12-12	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7C7Q	-	3.0	B	Active	-	71	-	-	-	-	-	-	(-)-baclofen BHFF	small-molecule small-molecule	Agonist PAM	-	-	No	No	Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y	10.1038/S41422-020-0350-5	2020-07-01	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6S0Q	6S0Q_refined	2.7	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	-	-	2020-07-15	Yes
5HT1B	5-HT_1B	5-Hydroxytryptamine	A	Human	X-ray	7C61	7C61_refined	3.0	A	Inactive	14	68	-	-	-	-	BRIL	IgG heavy chain IgG light chain	ergotamine	small-molecule	Antagonist	tryptamine, 5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI	10.1038/S41598-020-68355-X	2020-07-29	Yes
OXYR	OT	Vasopressin and oxytocin	A	Human	X-ray	6TPK	6TPK_refined	3.2	A	Inactive	14	68	-	-	-	-	GlgA glycogen synthase	-	retosiban	small-molecule	Antagonist	oxytocin, vasopressin	peptide	Yes	No	Waltenspuhl Y, Schoppe J, Ehrenmann J, Kummer L, Pluckthun A	10.1126/SCIADV.ABB5419	2020-08-05	Yes
SCTR	secretin	Glucagon	B1	Human	cryo-EM	6WI9	6WI9_refined	4.3	R	Active	100	84	Gs	αs	-	49	-	Nanobody-35	SECRETIN	protein	Agonist	secretin, VIP	peptide	No	No	Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ	10.1038/S41467-020-17791-4	2020-08-12	Yes
CXCR2	CXCR2	Chemokine	A	Human	X-ray	6LFL	6LFL_refined	3.2	A	Inactive	4	76	-	-	-	-	GlgA glycogen synthase	-	4-[[3,4-Dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide	small-molecule	Allosteric antagonist	CXCL7, CXCL8, CXCL6, CXCL2, CXCL1, CXCL5, CXCL3	peptide	No	No	Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ	10.1038/S41586-020-2492-5	2020-09-02	Yes
CXCR2	CXCR2	Chemokine	A	Human	cryo-EM	6LFM	6LFM_refined	3.5	R	Active	100	85	Gi/o	αi1	-	65	-	scFv16	Interleukin-8	protein	Agonist	CXCL7, CXCL8, CXCL6, CXCL2, CXCL1, CXCL5, CXCL3	peptide	No	No	Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ	10.1038/S41586-020-2492-5	2020-09-02	Yes
GPBAR	GPBA	Bile acid	A	Human	cryo-EM	7CFN	7CFN_refined	3.0	R	Active	100	83	Gs	αs	-	59	-	Nanobody-35	INT-777 INT-777	small-molecule small-molecule	Agonist PAM	lithocholic acid, chenodeoxycholic acid, cholic acid, deoxycholic acid	small-molecule	No	No	Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y	10.1038/S41586-020-2569-1	2020-09-09	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	3OE6	-	3.2	A	Inactive	3	77	-	-	-	-	T4-Lysozyme	-	isothiourea-1t	small-molecule	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC	10.1126/SCIENCE.1194396	2010-10-27	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	3OE9	-	3.1	A	Inactive	3	74	-	-	-	-	T4-Lysozyme	-	isothiourea-1t	small-molecule	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC	10.1126/SCIENCE.1194396	2010-10-27	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2Y03	2Y03_refined	2.9	B	Inactive	0	62	-	-	-	-	-	-	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG	10.1038/NATURE09746	2011-01-12	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3P0G	3P0G_refined	3.5	A	Active	100	69	-	-	-	-	T4-Lysozyme	Nanobody	CHEMBL1615159	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Rasmussen SG, Choi HJ, Fung JJ, Pardon E, Casarosa P, Chae PS, Devree BT, Rosenbaum DM, Thian FS, Kobilka TS, Schnapp A, Konetzki I, Sunahara RK, Gellman SH, Pautsch A, Steyaert J, Weis WI, Kobilka BK	10.1038/NATURE09648	2011-01-19	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	2YDO	2YDO_refined	3.0	A	Active	74	73	-	-	-	-	-	-	adenosine	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG	10.1038/NATURE10136	2011-05-18	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2YCX	-	3.3	A	Inactive	0	59	-	-	-	-	-	-	(S)-Cyanopindolol	small-molecule	Antagonist	-	-	Yes	No	Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF	10.1073/PNAS.1100185108	2011-06-01	Yes
HRH1	H₁	Histamine	A	Human	X-ray	3RZE	3RZE_refined	3.1	A	Inactive	3	55	-	-	-	-	T4-Lysozyme	-	doxepin	small-molecule	Antagonist	histamine	small-molecule	Yes	No	Shimamura T, Shiroishi M, Weyand S, Tsujimoto H, Winter G, Katritch V, Abagyan R, Cherezov V, Liu W, Han GW, Kobayashi T, Stevens RC, Iwata S	10.1038/NATURE10236	2011-06-15	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3PWH	-	3.3	A	Inactive	1	71	-	-	-	-	-	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH	10.1016/J.STR.2011.06.014	2011-09-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4A4M	4A4M_refined	3.3	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J	10.1073/PNAS.1114089108	2012-01-25	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	X-ray	3V2W	-	3.4	A	Inactive	1	68	-	-	-	-	T4-Lysozyme	-	W146	small-molecule	Antagonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC	10.1126/SCIENCE.1215904	2012-02-15	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3UZC	3UZC_refined	3.3	A	Inactive	1	71	-	-	-	-	-	-	CHEMBL2024114	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH.	10.1021/jm201376w	2012-03-21	Yes
OPRX	NOP	Opioid	A	Human	X-ray	4EA3	4EA3_refined	3.0	A	Inactive	3	75	-	-	-	-	BRIL	-	compound 24 [PMID: 16451050]	small-molecule	Antagonist	nociceptin/orphanin FQ	peptide	Yes	No	Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC	10.1038/NATURE11085	2012-04-25	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	4EIY	4EIY_refined	1.8	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Liu W, Chun E, Thompson AA, Chubukov P, Xu F, Katritch V, Han GW, Roth CB, Heitman LH, IJzerman AP, Cherezov V, Stevens RC	10.1126/SCIENCE.1219218	2012-07-25	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	4GPO	4GPO_refined	3.5	B	Inactive	0	58	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Huang J, Chen S, Zhang JJ, Huang XY	10.1038/NSMB.2504	2013-02-27	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	4IB4	4IB4_refined	2.7	A	Intermediate	42	59	-	-	-	-	BRIL	-	ergotamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC	10.1126/science.1232808	2013-03-13	Yes
SMO	SMO	Frizzled	F	Human	X-ray	4JKV	4JKV_refined	2.5	A	Inactive	0	44	-	-	-	-	BRIL	-	taladegib	small-molecule	Antagonist	-	-	No	No	Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC	10.1038/NATURE12167	2013-04-24	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	4LDL	4LDL_refined	3.1	A	Active	100	69	-	-	-	-	T4-Lysozyme	Nanobody	hydroxybenzylisoproterenol	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK	10.1038/NATURE12572	2013-09-25	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	4MQT	4MQT_refined	3.7	A	Active	99	59	-	-	-	-	-	Nanobody	iperoxo LY2119620	small-molecule small-molecule	Agonist PAM	acetylcholine	small-molecule	Yes	No	Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK	10.1038/NATURE12735	2013-11-27	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	3ZEV	-	3.0	A	Inactive	2	72	-	-	-	-	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A	10.1073/PNAS.1317903111	2014-01-29	Yes
SMO	SMO	Frizzled	F	Human	X-ray	4O9R	4O9R_refined	3.2	A	Inactive	11	42	-	-	-	-	BRIL	-	cyclopamine	small-molecule	Antagonist	-	-	No	No	Weierstall U, James D, Wang C, White TA, Wang D, Liu W, Spence JC, Bruce Doak R, Nelson G, Fromme P, Fromme R, Grotjohann I, Kupitz C, Zatsepin NA, Liu H, Basu S, Wacker D, Han GW, Katritch V, Boutet S, Messerschmidt M, Williams GJ, Koglin JE, Marvin Seibert M, Klinker M, Gati C, Shoeman RL, Barty A, Chapman HN, Kirian RA, Beyerlein KR, Stevens RC, Li D, Shah ST, Howe N, Caffrey M, Cherezov V	10.1038/NCOMMS4309	2014-03-05	Yes
P2Y12	P2Y₁₂	P2Y	A	Human	X-ray	4PXZ	4PXZ_refined	2.5	A	Intermediate	42	84	-	-	-	-	BRIL	-	2MeSADP	small-molecule	Agonist	ATP, ADP	small-molecule	Yes	No	Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q	10.1038/NATURE13288	2014-04-30	Yes
SMO	SMO	Frizzled	F	Human	X-ray	4QIM	4QIM_refined	2.6	A	Inactive	7	45	-	-	-	-	BRIL	-	ANTA XV	small-molecule	Antagonist	-	-	No	No	Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC	10.1038/NCOMMS5355	2014-07-23	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Rat	X-ray	4U14	4U14_refined	3.6	A	Inactive	3	47	-	-	-	-	T4-Lysozyme	-	tiotropium	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Thorsen TS, Matt R, Weis WI, Kobilka BK	10.1016/J.STR.2014.08.022	2014-11-26	Yes
OPRD	δ	Opioid	A	Human	X-ray	4RWD	4RWD_refined	2.7	A	Inactive	3	79	-	-	-	-	BRIL	-	DIPP-NH2	peptide	Antagonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	Yes	Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwe D, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V	10.1038/NSMB.2965	2015-01-14	Yes
P2RY1	P2Y₁	P2Y	A	Human	X-ray	4XNV	-	2.2	A	Intermediate	42	78	-	-	-	-	Rubredoxin	-	BMS compound 16 [PMID:23368907]	small-molecule	NAM	ATP, ADP	small-molecule	Yes	No	Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B	10.1038/NATURE14287	2015-04-01	Yes
P2RY1	P2Y₁	P2Y	A	Human	X-ray	4XNW	4XNW_refined	2.7	A	Intermediate	42	78	-	-	-	-	Rubredoxin	-	MRS2500	small-molecule	Antagonist	ATP, ADP	small-molecule	Yes	No	Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B	10.1038/NATURE14287	2015-04-01	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	4YAY	4YAY_refined	2.9	A	Inactive	3	79	-	-	-	-	BRIL	-	ZD-7155	small-molecule	Antagonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Zhang H, Unal H, Gati C, Han GW, Liu W, Zatsepin NA, James D, Wang D, Nelson G, Weierstall U, Sawaya MR, Xu Q, Messerschmidt M, Williams GJ, Boutet S, Yefanov OM, White TA, Wang C, Ishchenko A, Tirupula KC, Desnoyer R, Coe J, Conrad CE, Fromme P, Stevens RC, Katritch V, Karnik SS, Cherezov V	10.1016/J.CELL.2015.04.011	2015-04-22	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	X-ray	4Z36	4Z36_refined	2.9	A	Inactive	1	79	-	-	-	-	BRIL	-	ONO-3080573	small-molecule	Antagonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA	10.1016/J.CELL.2015.06.002	2015-06-03	Yes
OPSD	Rhodopsin	Opsins	A	Human	X-ray	4ZWJ	4ZWJ_refined	3.3	A	Active	100	94	Visual	S-arrestin	-	86	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Kang Y, Zhou XE, Gao X, He Y, Liu W, Ishchenko A, Barty A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Ke J, Tan MH, Zhang C, Moeller A, West GM, Pascal BD, Van Eps N, Caro LN, Vishnivetskiy SA, Lee RJ, Suino-Powell KM, Gu X, Pal K, Ma J, Zhi X, Boutet S, Williams GJ, Messerschmidt M, Gati C, Zatsepin NA, Wang D, James D, Basu S, Roy-Chowdhury S, Conrad CE, Coe J, Liu H, Lisova S, Kupitz C, Grotjohann I, Fromme R, Jiang Y, Tan M, Yang H, Li J, Wang M, Zheng Z, Li D, Howe N, Zhao Y, Standfuss J, Diederichs K, Dong Y, Potter CS, Carragher B, Caffrey M, Jiang H, Chapman HN, Spence JC, Fromme P, Weierstall U, Ernst OP, Katritch V, Gurevich VV, Griffin PR, Hubbell WL, Stevens RC, Cherezov V, Melcher K, Xu HE	10.1038/NATURE14656	2015-07-29	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	4ZJ8	4ZJ8_refined	2.8	A	Inactive	1	72	-	-	-	-	GlgA glycogen synthase	-	suvorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM	10.1038/NSMB.3183	2016-03-09	Yes
OPSD	Rhodopsin	Opsins	A	Human	X-ray	5DGY	5DGY_refined	7.7	A	Active	100	94	Visual	S-arrestin	-	86	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhou XE, Gao X, Barty A, Kang Y, He Y, Liu W, Ishchenko A, White TA, Yefanov O, Han GW, Xu Q, de Waal PW, Suino-Powell KM, Boutet S, Williams GJ, Wang M, Li D, Caffrey M, Chapman HN, Spence JC, Fromme P, Weierstall U, Stevens RC, Cherezov V, Melcher K, Xu HE	10.1038/SDATA.2016.21	2016-03-23	Yes
SMO	SMO	Frizzled	F	Human	X-ray	5L7I	5L7I_refined	3.3	B	Inactive	4	59	-	-	-	-	BRIL	-	vismodegib	small-molecule	Antagonist	-	-	No	No	Byrne EFX, Sircar R, Miller PS, Hedger G, Luchetti G, Nachtergaele S, Tully MD, Mydock-McGrane L, Covey DF, Rambo RP, Sansom MSP, Newstead S, Rohatgi R, Siebold C	10.1038/NATURE18934	2016-07-20	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	5GLH	5GLH_refined	2.8	A	Inactive	14	66	-	-	-	-	T4-Lysozyme	-	ENDOTHELIN	protein	Agonist	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T	10.1038/nature19319	2016-09-07	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	5TGZ	5TGZ_refined	2.8	A	Inactive	9	61	-	-	-	-	Flavodoxin	-	AM6538	small-molecule	Antagonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ	10.1016/J.CELL.2016.10.004	2016-11-02	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	5T04	5T04_refined	3.3	A	Active	92	69	-	-	-	-	T4-Lysozyme	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Krumm BE, Lee S, Bhattacharya S, Botos I, White CF, Du H, Vaidehi N, Grisshammer R	10.1038/SREP38564	2016-12-21	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	5TE3	5TE3_refined	2.7	A	Active	97	94	-	-	-	-	-	-	B-Octylglucoside	small-molecule	unknown	-	-	No	No	Gulati S, Jastrzebska B, Banerjee S, Placeres AL, Miszta P, Gao S, Gunderson K, Tochtrop GP, Filipek S, Katayama K, Kiser PD, Mogi M, Stewart PL, Palczewski K	10.1073/PNAS.1617446114	2017-03-15	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	5UNH	5UNH_refined	2.9	B	Active	99	75	-	-	-	-	BRIL	-	compound 2 [PMID: 28379944]	small-molecule	Antagonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Zhang H, Han GW, Batyuk A, Ishchenko A, White KL, Patel N, Sadybekov A, Zamlynny B, Rudd MT, Hollenstein K, Tolstikova A, White TA, Hunter MS, Weierstall U, Liu W, Babaoglu K, Moore EL, Katz RD, Shipman JM, Garcia-Calvo M, Sharma S, Sheth P, Soisson SM, Stevens RC, Katritch V, Cherezov V	10.1038/NATURE22035	2017-04-05	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	5UZ7	5UZ7_refined	4.1	R	Active	100	56	Gs	αs	-	47	-	-	-	-	-	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM	10.1038/NATURE22327	2017-05-03	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	5VEW	5VEW_refined	2.7	A	Inactive	0	57	-	-	-	-	T4-Lysozyme	-	PF-06372222	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC	10.1038/NATURE22378	2017-05-24	Yes
GLR	glucagon	Glucagon	B1	Human	X-ray	5XF1	5XF1_refined	3.2	B	Inactive	0	81	-	-	-	-	T4-Lysozyme	Antibody	NNC0640	small-molecule	NAM	glucagon	peptide	No	No	Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW, Grant TD, Sierra RG, Weierstall U, Nelson G, Liu W, Wu Y, Ma L, Cai X, Lin G, Wu X, Geng Z, Dong Y, Song G, Griffin PR, Lau J, Cherezov V, Yang H, Hanson MA, Stevens RC, Zhao Q, Jiang H, Wang MW, Wu B	10.1038/NATURE22363	2017-05-24	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	5NX2	-	3.7	A	Intermediate	30	84	-	-	-	-	-	-	Truncated protein agonist	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Jazayeri A, Rappas M, Brown AJH, Kean J, Errey JC, Robertson NJ, Fiez-Vandal C, Andrews SP, Congreve M, Bortolato A, Mason JS, Baig AH, Teobald I, Dore AS, Weir M, Cooke RM, Marshall FH	10.1038/NATURE22800	2017-06-14	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5MZJ	5MZJ_refined	2.0	A	Inactive	1	71	-	-	-	-	BRIL	-	theophylline	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM	10.1016/j.str.2017.06.012	2017-07-26	Yes
AA1R	A₁	Adenosine	A	Human	X-ray	5N2S	5N2S_refined	3.3	A	Inactive	1	86	-	-	-	-	BRIL	-	PSB36	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM	10.1016/j.str.2017.06.012	2017-07-26	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	5X93	5X93_refined	2.2	A	Inactive	5	71	-	-	-	-	T4-Lysozyme	-	K-8794	small-molecule	Antagonist	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O	10.1038/NSMB.3450	2017-08-16	Yes
Q08BG4	LPA₆	Lysophospholipid (LPA)	A	Zebrafish	X-ray	5XSZ	5XSZ_refined	3.2	A	Intermediate	42	78	-	-	-	-	T4-Lysozyme	-	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Taniguchi R, Inoue A, Sayama M, Uwamizu A, Yamashita K, Hirata K, Yoshida M, Tanaka Y, Kato HE, Nakada-Nakura Y, Otani Y, Nishizawa T, Doi T, Ohwada T, Ishitani R, Aoki J, Nureki O	10.1038/NATURE23448	2017-08-16	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5NM2	5NM2_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J	10.1038/S41467-017-00630-4	2017-09-27	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5VRA	5VRA_refined	2.4	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP	10.1038/NPROT.2017.135	2017-12-13	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OLG	5OLG_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OLZ	5OLZ_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL2024114	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
GLR	glucagon	Glucagon	B1	Human	X-ray	5YQZ	5YQZ_refined	3.0	R	Inactive	3	83	-	-	-	-	T4-Lysozyme	-	NNC1702	peptide	Agonist (partial)	glucagon	peptide	No	No	Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C, Cao C, He L, Yang H, Lau J, Ernst OP, Hanson MA, Stevens RC, Wang MW, Reedtz-Runge S, Jiang H, Zhao Q, Wu B	10.1038/NATURE25153	2018-01-17	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6B3J	6B3J_refined	3.3	R	Active	100	82	Gs	αs	-	49	-	-	Exendin-P5	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D	10.1038/NATURE25773	2018-02-21	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FKC	6FKC_refined	2.5	A	Active	97	94	-	-	-	-	-	-	3-[1'-[(2~{S})-2-(4-chlorophenyl)-3-methyl-butanoyl]spiro[1,3-benzodioxole-2,4'-piperidine]-5-yl]propanoic acid	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
AA2AR	A_2A	Adenosine	A	Human	cryo-EM	6GDG	6GDG_refined	4.1	A	Active	100	64	Gs	αs	-	57	TrxA	Nanobody-35	NECA	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Garcia-Nafria J, Lee Y, Bai X, Carpenter B, Tate CG	10.7554/ELIFE.35946	2018-05-16	Yes
Q80KM9	US28	Unclassified	A	strain AD169	X-ray	5WB2	5WB2_refined	3.5	A	Active	99	82	-	-	-	-	-	Nanobody	CX₃CL1	peptide	Agonist	-	-	Yes	No	Miles TF, Spiess K, Jude KM, Tsutsumi N, Burg JS, Ingram JR, Waghray D, Hjorto GM, Larsen O, Ploegh HL, Rosenkilde MM, Garcia KC	10.7554/ELIFE.35850	2018-06-13	Yes
5HT1B	5-HT_1B	5-Hydroxytryptamine	A	Human	cryo-EM	6G79	6G79_refined	3.8	S	Active	100	67	Gi/o	αo	-	59	-	-	donitriptan	small-molecule	Agonist	tryptamine, 5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	Garcia-Nafria J, Nehme R, Edwards PC, Tate CG	10.1038/S41586-018-0241-9	2018-06-20	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	6DRZ	6DRZ_refined	3.1	A	Intermediate	42	61	-	-	-	-	BRIL	-	methysergide	small-molecule	Antagonist	5-hydroxytryptamine	small-molecule	Yes	No	McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL	10.1038/s41594-018-0116-7	2018-08-29	Yes
PD2R2	DP₂	Prostanoid	A	Human	X-ray	6D27	6D27_refined	2.7	A	Inactive	24	81	-	-	-	-	T4-Lysozyme	-	CHEMBL179036	small-molecule	Antagonist	PGJ₂, PGD₂, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C	10.1016/J.MOLCEL.2018.08.009	2018-10-03	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6H7J	6H7J_refined	2.8	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb80	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG	10.1126/SCIENCE.AAU5595	2018-10-17	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6H7N	6H7N_refined	2.5	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb6B9	(S)-Xamoterol	small-molecule	Agonist	-	-	Yes	No	-	10.1101/436212	2018-10-17	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	5YC8	5YC8_refined	2.5	A	Inactive	3	60	-	-	-	-	BRIL	-	N-methyl scopolamine	small-molecule	Antagonist	acetylcholine	small-molecule	No	No	Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T	10.1038/S41589-018-0152-Y	2018-11-21	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	5ZKB	5ZKB_refined	3.0	A	Inactive	3	60	-	-	-	-	BRIL	-	AF-DX 384	small-molecule	Antagonist	acetylcholine	small-molecule	No	No	Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T	10.1038/S41589-018-0152-Y	2018-11-21	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	6IGL	-	2.7	A	Inactive	5	70	-	-	-	-	T4-Lysozyme	-	IRL 1620	peptide	Agonist (partial)	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T, Nureki O	10.1038/S41467-018-07094-0	2018-11-21	Yes
PE2R3	EP₃	Prostanoid	A	Human	X-ray	6AK3	6AK3_refined	2.9	B	Active	92	69	-	-	-	-	BRIL	-	PGE₂	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Morimoto K, Suno R, Hotta Y, Yamashita K, Hirata K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T	10.1038/S41589-018-0171-8	2018-12-05	Yes
TA2R	TP	Prostanoid	A	Human	X-ray	6IIU	6IIU_refined	2.5	A	Intermediate	42	87	-	-	-	-	Rubredoxin	-	ramatroban	small-molecule	Antagonist	PGD₂, thromboxane A₂, PGE₂, PGF_2α, PGI₂, PGH₂	small-molecule	No	No	Fan H, Chen S, Yuan X, Han S, Zhang H, Xia W, Xu Y, Zhao Q, Wu B	10.1038/S41589-018-0170-9	2018-12-19	Yes
CCR2	CCR2	Chemokine	A	Human	X-ray	6GPS	6GPS_refined	3.3	A	Inactive	16	74	-	-	-	-	Rubredoxin	-	MK-0812	small-molecule	Antagonist	CCL24, CCL2, CCL26, CCL8, CCL13, CCL7, CCL16, CCL11	peptide	No	No	Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G	10.1016/J.STR.2018.10.027	2019-01-02	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6IBL	6IBL_refined	2.7	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb80	arformoterol	small-molecule	Agonist	-	-	Yes	No	-	10.1101/436212	2019-01-09	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6HLO	6HLO_refined	2.4	A	Inactive	1	70	-	-	-	-	GlgA glycogen synthase	-	aprepitant	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A	10.1038/S41467-018-07939-8	2019-01-16	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	cryo-EM	6N51	6N51_refined	4.0	B	Intermediate	-	65	-	-	-	-	-	Nanobody-43	quisqualate	small-molecule	Agonist	L-glutamic acid	small-molecule	No	No	Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK	10.1038/S41586-019-0881-4	2019-01-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	6NIY	6NIY_refined	3.3	R	Active	100	55	Gs	αs	-	43	-	-	Calcitonin salmon	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM	10.1021/ACSPTSCI.8B00056	2019-01-23	Yes
CNR1	CB₁	Cannabinoid	A	Human	cryo-EM	6N4B	6N4B_refined	3.0	R	Active	100	58	Gi/o	αi1	-	62	-	scFv16	MDMB-Fubinaca	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G	10.1016/J.CELL.2018.11.040	2019-01-30	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6J20	6J20_refined	2.7	A	Inactive	1	71	-	-	-	-	T4-Lysozyme	-	aprepitant	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	No	No	Chen S, Lu M, Liu D, Yang L, Yi C, Ma L, Zhang H, Liu Q, Frimurer TM, Wang MW, Schwartz TW, Stevens RC, Wu B, Wuthrich K, Zhao Q	10.1038/S41467-019-08568-5	2019-03-06	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	6NBF	6NBF_refined	3.0	R	Active	100	62	Gs	αs	-	58	-	Nanobody-35	Long-acting parathyroid hormone analog	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y	10.1126/SCIENCE.AAV7942	2019-04-17	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	6NBI	6NBI_refined	4.0	R	Active	100	62	Gs	αs	-	56	-	Nanobody-35	Long-acting parathyroid hormone analog	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y	10.1126/SCIENCE.AAV7942	2019-04-17	Yes
MTR1A	MT₁	Melatonin	A	Human	X-ray	6ME5	6ME5_refined	3.2	A	Inactive	1	83	-	-	-	-	GlgA glycogen synthase	-	agomelatine	small-molecule	Agonist	melatonin	small-molecule	No	No	Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V	10.1038/S41586-019-1141-3	2019-04-24	Yes
MTR1B	MT₂	Melatonin	A	Human	X-ray	6ME7	6ME7_refined	3.2	A	Inactive	1	79	-	-	-	-	Rubredoxin	-	2-phenylmelatonin	small-molecule	Agonist	melatonin	small-molecule	No	No	Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V	10.1038/S41586-019-1144-0	2019-04-24	Yes
MTR1B	MT₂	Melatonin	A	Human	X-ray	6ME9	6ME9_refined	3.3	B	Inactive	1	79	-	-	-	-	Rubredoxin	-	ramelteon	small-molecule	Agonist	melatonin	small-molecule	No	No	Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V	10.1038/S41586-019-1144-0	2019-04-24	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	cryo-EM	6OIJ	6OIJ_refined	3.3	R	Active	100	64	Gq/11	α11	-	63	-	Antibody fragment	iperoxo	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK	10.1126/SCIENCE.AAW5188	2019-05-08	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6E67	6E67_refined	3.7	B	Active	100	72	Gs	αs	Fused partial Gs	44	T4-Lysozyme	-	CHEMBL1615159	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK	10.1016/J.CELL.2019.04.021	2019-06-05	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6GT3	6GT3_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	imaradenant	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	-	-	2019-06-26	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6N48	6N48_refined	3.2	A	Active	100	70	-	-	-	-	T4-Lysozyme	Camelid Antibody Fragment	CHEMBL1615159 2-[[(3R)-4-(4-Tert-butylphenyl)-3-[[2-(4-methoxyphenyl)sulfanyl-5-[methyl(propan-2-yl)sulfamoyl]benzoyl]amino]butanoyl]amino]acetic acid	small-molecule small-molecule	Agonist PAM	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Liu X, Masoudi A, Kahsai AW, Huang LY, Pani B, Staus DP, Shim PJ, Hirata K, Simhal RK, Schwalb AM, Rambarat PK, Ahn S, Lefkowitz RJ, Kobilka B	10.1126/SCIENCE.AAW8981	2019-06-26	Yes
SMO	SMO	Frizzled	F	Mouse	X-ray	6O3C	6O3C_refined	2.8	A	Active	95	61	-	-	-	-	-	Nanobody-Smo8	SAG21k	small-molecule	Agonist	-	-	No	No	Deshpande I, Liang J, Hedeen D, Roberts KJ, Zhang Y, Ha B, Latorraca NR, Faust B, Dror RO, Beachy PA, Myers BR, Manglik A	10.1038/S41586-019-1355-4	2019-07-03	Yes
NTR1	NTS₁	Neurotensin	A	Human	cryo-EM	6OSA	6OSA_refined	3.0	R	Active	100	77	Gi/o	αi1	Non-canonical conformation	62	-	-	JMV449	peptide	Agonist	large neuromedin N, neurotensin, neuromedin N, large neurotensin	peptide	Yes	No	Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G	10.1038/S41586-019-1337-6	2019-07-10	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	6K1Q	6K1Q_refined	2.7	A	Inactive	5	68	-	-	-	-	T4-Lysozyme	-	IRL 2500	peptide	Inverse agonist	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Nagiri C, Shihoya W, Inoue A, Kadji FMN, Aoki J, Nureki O	10.1038/S42003-019-0482-7	2019-07-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	6OYA	6OYA_refined	3.3	R	Active	100	94	Gi/o	αt1	-	59	-	Camelid antibody VHH fragment	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G	10.1016/J.MOLCEL.2019.06.007	2019-07-24	Yes
SUCR1	succinate	Succinate	A	Rat	X-ray	6RNK	6RNK_refined	1.9	A	Intermediate	42	90	-	-	-	-	-	Nanobody-6	NF-56-EJ40	small-molecule	Antagonist	-	-	Yes	No	Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP	10.1038/S41586-019-1663-8	2019-08-14	Yes
CCR7	CCR7	Chemokine	A	Human	X-ray	6QZH	6QZH_refined	2.1	A	Inactive	4	71	-	-	-	-	Sialidase NanA	-	SCHEMBL13407377	small-molecule	Allosteric antagonist	CCL21, CCL19	peptide	No	No	Jaeger K, Bruenle S, Weinert T, Guba W, Muehle J, Miyazaki T, Weber M, Furrer A, Haenggi N, Tetaz T, Huang CY, Mattle D, Vonach JM, Gast A, Kuglstatter A, Rudolph MG, Nogly P, Benz J, Dawson RJP, Standfuss J	10.1016/J.CELL.2019.07.028	2019-09-04	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6JZH	6JZH_refined	2.3	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Shimazu Y, Tono K, Tanaka T, Yamanaka Y, Nakane T, Mori C, Terakado Kimura K, Fujiwara T, Sugahara M, Tanaka R, Doak RB, Shimamura T, Iwata S, Nango E, Yabashi M	10.1107/S1600576719012846	2019-10-30	Yes
CLTR1	CysLT₁	Leukotriene	A	Human	X-ray	6RZ5	6RZ5_refined	2.5	B	Intermediate	42	84	-	-	-	-	BRIL	-	zafirlukast	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	Yes	Yes	Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V	10.1126/SCIADV.AAX2518	2019-10-30	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	6KK1	6KK1_refined	2.8	B	Inactive	0	57	-	-	-	-	T4-Lysozyme	-	PF-06372222	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G	10.1107/S2052252519013496	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PRZ	6PRZ_refined	2.8	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	CHEMBL1160734	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS1	6PS1_refined	3.2	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	timolol	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS3	6PS3_refined	2.5	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	CHEMBL3799125	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS5	6PS5_refined	2.9	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	propranolol	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6PS7	6PS7_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	cryo-EM	6NI3	6NI3_refined	3.8	R	Active	100	69	Gs	αs	-	59	-	Nanobody-35	CHEMBL1615159	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ	10.1038/S41594-019-0330-Y	2019-11-20	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	X-ray	6KUX	6KUX_refined	2.7	A	Inactive	1	57	-	-	-	-	BRIL	-	RSC	small-molecule	Antagonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2019-12-04	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	X-ray	6KUY	6KUY_refined	3.2	A	Inactive	1	56	-	-	-	-	BRIL	-	(2~{S})-4-fluoranyl-2-(1~{H}-imidazol-5-yl)-1-propan-2-yl-2,3-dihydroindole	small-molecule	Agonist (partial)	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2019-12-04	Yes
ACM5	M₅	Acetylcholine (muscarinic)	A	Human	X-ray	6OL9	6OL9_refined	2.5	A	Inactive	3	53	-	-	-	-	T4-Lysozyme	-	tiotropium	small-molecule	Inverse agonist	acetylcholine	small-molecule	No	No	Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM	10.1073/PNAS.1914446116	2019-12-11	Yes
OPRD	δ	Opioid	A	Human	X-ray	6PT3	6PT3_refined	3.3	A	Active	74	78	-	-	-	-	BRIL	-	DPI-287	small-molecule	Agonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	No	No	Claff T, Yu J, Blais V, Patel N, Martin C, Wu L, Han GW, Holleran BJ, Van der Poorten O, White KL, Hanson MA, Sarret P, Gendron L, Cherezov V, Katritch V, Ballet S, Liu ZJ, Muller CE, Stevens RC	10.1126/SCIADV.AAX9115	2019-12-11	Yes
CLTR2	CysLT₂	Leukotriene	A	Human	X-ray	6RZ6	6RZ6_refined	2.4	A	Intermediate	42	82	-	-	-	-	BRIL	-	ONO-2570366	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	No	No	Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V	10.1038/S41467-019-13348-2	2019-12-11	Yes
CLTR2	CysLT₂	Leukotriene	A	Human	X-ray	6RZ8	6RZ8_refined	2.7	A	Intermediate	42	78	-	-	-	-	BRIL	-	ONO-2080365	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	No	No	Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V	10.1038/S41467-019-13348-2	2019-12-11	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TO7	-	2.3	A	Inactive	1	71	-	-	-	-	-	-	suvorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TP3	6TP3_refined	3.0	A	Inactive	1	74	-	-	-	-	-	-	daridorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TP6	6TP6_refined	2.3	B	Inactive	1	71	-	-	-	-	-	-	filorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	6TPN	6TPN_refined	2.6	A	Inactive	1	71	-	-	-	-	GlgA glycogen synthase	-	HTL6641	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TQ4	6TQ4_refined	2.3	B	Inactive	1	70	-	-	-	-	-	-	CHEMBL4590386	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
CXCR4	CXCR4	Chemokine	A	Human	X-ray	3OE8	-	3.1	A	Inactive	3	76	-	-	-	-	T4-Lysozyme	-	isothiourea-1t	small-molecule	Antagonist	CXCL12ε, CXCL12β, CXCL12φ, CXCL12α, CXCL12, CXCL12γ, CXCL12δ	peptide	Yes	No	Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC	10.1126/SCIENCE.1194396	2010-10-27	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2Y04	2Y04_refined	3.1	B	Inactive	0	62	-	-	-	-	-	-	levosalbutamol	small-molecule	Agonist (partial)	-	-	Yes	No	Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG	10.1038/NATURE09746	2011-01-12	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	3PQR	-	2.9	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP	10.1038/NATURE09789	2011-03-09	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3QAK	3QAK_refined	2.7	A	Active	74	69	-	-	-	-	T4-Lysozyme	-	UK-432,097	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Xu F, Wu H, Katritch V, Han GW, Jacobson KA, Gao ZG, Cherezov V, Stevens RC	10.1126/SCIENCE.1202793	2011-03-09	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	2YCZ	2YCZ_refined	3.7	B	Inactive	0	60	-	-	-	-	-	-	Iodocyanopindolol	small-molecule	Antagonist	-	-	Yes	No	Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF	10.1073/PNAS.1100185108	2011-06-01	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	3SN6	3SN6_refined	3.2	R	Active	100	69	Gs	αs	-	89	T4-Lysozyme	Antibody	CHEMBL1615159	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK	10.1038/NATURE10361	2011-07-20	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	3VG9	3VG9_refined	2.7	A	Inactive	1	72	-	-	-	-	-	Antibody fab fragment light chain Antibody fab fragment heavy chain	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Hino T, Arakawa T, Iwanari H, Yurugi-Kobayashi T, Ikeda-Suno C, Nakada-Nakura Y, Kusano-Arai O, Weyand S, Shimamura T, Nomura N, Cameron AD, Kobayashi T, Hamakubo T, Iwata S, Murata T	10.1038/NATURE10750	2012-02-01	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Rat	X-ray	4DAJ	-	3.4	A	Inactive	3	46	-	-	-	-	T4-Lysozyme	-	tiotropium	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Kruse AC, Hu J, Pan AC, Arlow DH, Rosenbaum DM, Rosemond E, Green HF, Liu T, Chae PS, Dror RO, Shaw DE, Weis WI, Wess J, Kobilka BK	10.1038/NATURE10867	2012-02-22	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	4AMI	4AMI_refined	3.2	A	Inactive	0	58	-	-	-	-	-	-	Bucindolol	small-molecule	Agonist	-	-	Yes	No	Warne T, Edwards PC, Leslie AG, Tate CG	10.1016/J.STR.2012.03.014	2012-05-23	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	4GBR	4GBR_refined	4.0	A	Inactive	0	69	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Zou Y, Weis WI, Kobilka BK	10.1371/JOURNAL.PONE.0046039	2012-10-24	Yes
5HT1B	5-HT_1B	5-Hydroxytryptamine	A	Human	X-ray	4IAR	4IAR_refined	2.7	A	Inactive	14	70	-	-	-	-	BRIL	-	ergotamine	small-molecule	Agonist	tryptamine, 5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE	10.1126/SCIENCE.1232807	2013-03-13	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4BEZ	-	3.3	A	Active	97	94	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J	10.1038/EMBOR.2013.44	2013-04-24	Yes
CRFR1	CRF₁	Corticotropin-releasing factor	B1	Human	X-ray	4K5Y	-	3.0	C	Inactive	16	60	-	-	-	-	T4-Lysozyme	-	CP 376,395	small-molecule	Antagonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2	peptide	No	No	Hollenstein K, Kean J, Bortolato A, Cheng RK, Dore AS, Jazayeri A, Cooke RM, Weir M, Marshall FH	10.1038/NATURE12357	2013-07-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4J4Q	4J4Q_refined	2.7	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	B-Octylglucoside	small-molecule	unknown	-	-	No	No	Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP	10.1002/ANIE.201302374	2013-10-30	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	4NC3	4NC3_refined	2.8	A	Intermediate	42	60	-	-	-	-	BRIL	-	ergotamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Liu W, Wacker D, Gati C, Han GW, James D, Wang D, Nelson G, Weierstall U, Katritch V, Barty A, Zatsepin NA, Li D, Messerschmidt M, Boutet S, Williams GJ, Koglin JE, Seibert MM, Wang C, Shah ST, Basu S, Fromme R, Kupitz C, Rendek KN, Grotjohann I, Fromme P, Kirian RA, Beyerlein KR, White TA, Chapman HN, Caffrey M, Spence JC, Stevens RC, Cherezov V	10.1126/SCIENCE.1244142	2013-12-18	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4BUO	4BUO_refined	2.8	A	Inactive	2	72	-	-	-	-	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Egloff P, Hillenbrand M, Klenk C, Batyuk A, Heine P, Balada S, Schlinkmann KM, Scott DJ, Schutz M, Pluckthun A	10.1073/PNAS.1317903111	2014-01-29	Yes
GRM1	mGlu₁	Metabotropic glutamate	C	Human	X-ray	4OR2	4OR2_refined	2.8	B	Inactive	-	22	-	-	-	-	BRIL	-	FITM	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC	10.1126/science.1249489	2014-03-19	Yes
FFAR1	FFA1	Free fatty acid	A	Human	X-ray	4PHU	4PHU_refined	2.3	A	Intermediate	42	90	-	-	-	-	T4-Lysozyme	-	fasiglifam	small-molecule	Agonist	docosahexaenoic acid, oleic acid, α-linolenic acid, myristic acid	small-molecule	No	No	Srivastava A, Yano J, Hirozane Y, Kefala G, Gruswitz F, Snell G, Lane W, Ivetac A, Aertgeerts K, Nguyen J, Jennings A, Okada K	10.1038/NATURE13494	2014-07-16	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	4PXF	4PXF_refined	2.8	A	Active	100	93	Visual	S-arrestin	Fragment	2	-	-	B-Octylglucoside	small-molecule	unknown	-	-	No	No	Szczepek M, Beyriere F, Hofmann KP, Elgeti M, Kazmin R, Rose A, Bartl FJ, von Stetten D, Heck M, Sommer ME, Hildebrand PW, Scheerer P	10.1038/NCOMMS5801	2014-09-17	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Rat	X-ray	4U15	4U15_refined	2.8	B	Inactive	3	47	-	-	-	-	T4-Lysozyme	-	tiotropium	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	Thorsen TS, Matt R, Weis WI, Kobilka BK	10.1016/J.STR.2014.08.022	2014-11-26	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	4S0V	4S0V_refined	2.5	A	Inactive	1	64	-	-	-	-	Glycogen synthase	-	suvorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	Yes	No	Yin J, Mobarec JC, Kolb P, Rosenbaum DM	10.1038/NATURE14035	2015-01-14	Yes
US28	US28	Unclassified	A	strain AD169	X-ray	4XT3	4XT3_refined	3.8	A	Active	99	81	-	-	-	-	-	-	CX₃CL1	peptide	Agonist (partial)	-	-	Yes	No	Burg JS, Ingram JR, Venkatakrishnan AJ, Jude KM, Dukkipati A, Feinberg EN, Angelini A, Waghray D, Dror RO, Ploegh HL, Garcia KC	10.1126/SCIENCE.AAA5026	2015-03-04	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	4UHR	4UHR_refined	2.6	A	Active	74	75	-	-	-	-	-	-	CGS 21680	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Lebon G, Edwards PC, Leslie AG, Tate CG	10.1124/mol.114.097360	2015-04-08	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	X-ray	4Z35	4Z35_refined	2.9	A	Inactive	1	80	-	-	-	-	BRIL	-	ONO-9910539	small-molecule	Antagonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M, Mizuno H, Griffith MT, Rodgers C, Han GW, Velasquez J, Chun J, Stevens RC, Hanson MA	10.1016/J.CELL.2015.06.002	2015-06-03	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	4XES	4XES_refined	2.6	A	Active	92	72	-	-	-	-	T4-Lysozyme	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Krumm BE, White JF, Shah P, Grisshammer R	10.1038/NCOMMS8895	2015-07-29	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	5CGD	5CGD_refined	2.6	A	Inactive	-	20	-	-	-	-	T4-Lysozyme	-	CHEMBL3603923	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M.	10.1021/acs.jmedchem.5b00892	2015-08-12	Yes
OPRX	NOP	Opioid	A	Human	X-ray	5DHH	5DHH_refined	3.0	A	Inactive	3	76	-	-	-	-	BRIL	-	SB 612111	small-molecule	Antagonist	nociceptin/orphanin FQ	peptide	Yes	No	Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC	10.1016/J.STR.2015.07.024	2015-10-21	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	5D5A	5D5A_refined	2.5	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Huang CY, Olieric V, Ma P, Howe N, Vogeley L, Liu X, Warshamanage R, Weinert T, Panepucci E, Kobilka B, Diederichs K, Wang M, Caffrey M	10.1107/S2059798315021683	2016-01-13	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	X-ray	5CXV	5CXV_refined	2.7	A	Inactive	3	62	-	-	-	-	T4-Lysozyme	-	0HK	small-molecule	Antagonist	acetylcholine	small-molecule	Yes	No	-	-	2016-03-09	Yes
CRFR1	CRF₁	Corticotropin-releasing factor	B1	Human	X-ray	4Z9G	-	3.2	A	Inactive	16	63	-	-	-	-	T4-Lysozyme	-	CP 376,395	small-molecule	Antagonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2	peptide	No	No	Dore AS, Bortolato A, Hollenstein K, Cheng RKY, Read RJ, Marshall FH	10.2174/1874467210666170110114727	2016-06-29	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5IUA	5IUA_refined	2.2	A	Inactive	1	72	-	-	-	-	BRIL	-	2-(Furan-2-yl)-5-N-[3-(4-phenylpiperazin-1-yl)propyl]-1H-[1,2,4]triazolo[1,5-a][1,3,5]triazin-8-ium-5,7-diamine	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Segala E, Guo D, Cheng RK, Bortolato A, Deflorian F, Doré AS, Errey JC, Heitman LH, IJzerman AP, Marshall FH, Cooke RM.	10.1021/acs.jmedchem.6b00653	2016-06-29	Yes
SMO	SMO	Frizzled	F	Human	X-ray	5L7D	5L7D_refined	3.2	B	Inactive	4	59	-	-	-	-	BRIL	-	-	-	-	-	-	No	No	Byrne EFX, Sircar R, Miller PS, Hedger G, Luchetti G, Nachtergaele S, Tully MD, Mydock-McGrane L, Covey DF, Rambo RP, Sansom MSP, Newstead S, Rohatgi R, Siebold C	10.1038/NATURE18934	2016-07-20	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	5EN0	5EN0_refined	2.8	A	Active	100	94	Gi/o	αt3	Only H5	3	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J	10.15252/EMBR.201642671	2016-08-10	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5K2A	5K2A_refined	2.5	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V	10.1126/SCIADV.1600292	2016-09-21	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5K2D	5K2D_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Batyuk A, Galli L, Ishchenko A, Han GW, Gati C, Popov PA, Lee MY, Stauch B, White TA, Barty A, Aquila A, Hunter MS, Liang M, Boutet S, Pu M, Liu ZJ, Nelson G, James D, Li C, Zhao Y, Spence JC, Liu W, Fromme P, Katritch V, Weierstall U, Stevens RC, Cherezov V	10.1126/SCIADV.1600292	2016-09-21	Yes
CCR2	CCR2	Chemokine	A	Human	X-ray	5T1A	5T1A_refined	2.8	A	Inactive	16	76	-	-	-	-	T4-Lysozyme	-	CCR2-RA-[R] BMS-681	small-molecule small-molecule	Allosteric antagonist Antagonist	CCL24, CCL2, CCL26, CCL8, CCL13, CCL7, CCL16, CCL11	peptide	No	No	Zheng Y, Qin L, Zacarias NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM	10.1038/NATURE20605	2016-12-14	Yes
AA1R	A₁	Adenosine	A	Human	X-ray	5UEN	5UEN_refined	3.2	B	Inactive	1	91	-	-	-	-	BRIL	-	DU172	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jorg M, Scammells PJ, May LT, Sexton PM, Christopoulos A	10.1016/j.cell.2017.01.042	2017-03-01	Yes
PAR2	PAR2	Proteinase-activated	A	Human	X-ray	5NDD	5NDD_refined	2.8	A	Intermediate	42	74	-	-	-	-	BRIL	-	AZ8838	small-molecule	Antagonist	-	-	Yes	Yes	Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Dore AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundstrom L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N	10.1038/NATURE22309	2017-05-03	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	5VEX	5VEX_refined	3.0	B	Inactive	0	57	-	-	-	-	T4-Lysozyme	-	NNC0640	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC	10.1038/NATURE22378	2017-05-17	Yes
G1SGD4	GLP-1	Glucagon	B1	Rabbit	cryo-EM	5VAI	5VAI_refined	4.1	R	Active	100	84	Gs	αs	-	59	-	-	CHEMBL410972	protein	Agonist	-	-	No	No	Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G	10.1038/NATURE22394	2017-05-24	Yes
FFAR1	FFA1	Free fatty acid	A	Human	X-ray	5TZY	5TZY_refined	3.2	A	Intermediate	42	91	-	-	-	-	T4-Lysozyme	-	MK-8666 (2S,3R)-3-Cyclopropyl-3-[(2R)-2-[1-[(1S)-1-[5-fluoro-2-(trifluoromethoxy)phenyl]ethyl]piperidin-4-yl]-3,4-dihydro-2H-chromen-7-yl]-2-methylpropanoic acid	small-molecule small-molecule	Agonist PAM	docosahexaenoic acid, oleic acid, α-linolenic acid, myristic acid	small-molecule	No	No	Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM	10.1038/NSMB.3417	2017-06-07	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	5XRA	5XRA_refined	2.8	A	Active	96	60	-	-	-	-	Flavodoxin	-	AM11542	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ	10.1038/NATURE23272	2017-07-12	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5N2R	5N2R_refined	2.8	A	Inactive	1	71	-	-	-	-	BRIL	-	PSB36	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Cheng RKY, Segala E, Robertson N, Deflorian F, Dore AS, Errey JC, Fiez-Vandal C, Marshall FH, Cooke RM	10.1016/j.str.2017.06.012	2017-07-26	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	5X7D	5X7D_refined	2.7	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	4-carbamoyl-N-[(2R)-2-cyclohexyl-2-phenylacetyl]-L-phenylalanyl-3-bromo-N-methyl-L-phenylalaninamide Carazolol	small-molecule small-molecule	Allosteric antagonist Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Liu X, Ahn S, Kahsai AW, Meng KC, Latorraca NR, Pani B, Venkatakrishnan AJ, Masoudi A, Weis WI, Dror RO, Chen X, Lefkowitz RJ, Kobilka BK	10.1038/NATURE23652	2017-08-16	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5NLX	-	2.1	A	Inactive	1	73	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Weinert T, Olieric N, Cheng R, Brunle S, James D, Ozerov D, Gashi D, Vera L, Marsh M, Jaeger K, Dworkowski F, Panepucci E, Basu S, Skopintsev P, Dore AS, Geng T, Cooke RM, Liang M, Prota AE, Panneels V, Nogly P, Ermler U, Schertler G, Hennig M, Steinmetz MO, Wang M, Standfuss J	10.1038/S41467-017-00630-4	2017-09-27	Yes
DRD4	D₄	Dopamine	A	Human	X-ray	5WIU	-	2.0	A	Inactive	1	58	-	-	-	-	BRIL	-	[3H]NEMONAPRIDE	small-molecule	Antagonist	dopamine	small-molecule	Yes	No	Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang XP, Dror RO, Shoichet BK, Roth BL	10.1126/SCIENCE.AAN5468	2017-10-18	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	5WKT	5WKT_refined	3.2	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	B-Octylglucoside	small-molecule	unknown	-	-	No	No	Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP	10.1038/NPROT.2017.135	2017-12-13	Yes
C5AR1	C5a₁	Complement peptide	A	Human	X-ray	5O9H	5O9H_refined	2.7	A	Inactive	6	84	-	-	-	-	-	-	NDT9513727	small-molecule	Antagonist	C3a, C5a, C5a des-Arg, ribosomal protein S19	peptide	Yes	No	Robertson N, Rappas M, Dore AS, Brown J, Bottegoni G, Koglin M, Cansfield J, Jazayeri A, Cooke RM, Marshall FH	10.1038/NATURE25025	2018-01-10	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	5OLV	5OLV_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL1671936	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Rucktooa P, Cheng RKY, Segala E, Geng T, Errey JC, Brown GA, Cooke RM, Marshall FH, Dore AS	10.1038/S41598-017-18570-W	2018-01-17	Yes
OPRK	κ	Opioid	A	Human	X-ray	6B73	6B73_refined	3.1	A	Active	100	73	-	-	-	-	BRIL	Nanobody	MP1104	small-molecule	Agonist	big dynorphin, β-neoendorphin, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL	10.1016/J.CELL.2017.12.011	2018-01-17	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	X-ray	6BQH	6BQH_refined	2.7	A	Inactive	1	63	-	-	-	-	BRIL	-	ritanserin	small-molecule	Inverse agonist	5-hydroxytryptamine	small-molecule	Yes	No	Peng Y, McCorvy JD, Harpsoe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjorn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ	10.1016/j.cell.2018.01.001	2018-02-14	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	6FFH	6FFH_refined	2.7	A	Inactive	-	21	-	-	-	-	T4-Lysozyme	-	fenobam	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Christopher JA, Orgovan Z, Congreve M, Dore AS, Errey JC, Marshall FH, Mason JS, Okrasa K, Rucktooa P, Serrano-Vega MJ, Ferenczy GG, Keseru GM	10.1021/ACS.JMEDCHEM.7B01722	2018-03-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FK6	6FK6_refined	2.4	A	Active	97	94	-	-	-	-	-	-	COMPOUND SUMMARY	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FK9	6FK9_refined	2.6	A	Active	97	94	-	-	-	-	-	-	(2~{S})-3-methyl-2-phenyl-1-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-yl-butan-1-one	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6FKD	6FKD_refined	2.5	A	Active	97	94	-	-	-	-	-	-	5-chloro-2-(2-oxo-2-spiro[1,3-benzodioxole-2,4'-piperidine]-1'-ylethyl)-3H-pyridin-6-one	small-molecule	Agonist	-	-	No	No	Mattle D, Kuhn B, Aebi J, Bedoucha M, Kekilli D, Grozinger N, Alker A, Rudolph MG, Schmid G, Schertler GFX, Hennig M, Standfuss J, Dawson RJP	10.1073/PNAS.1718084115	2018-04-04	Yes
FFAR1	FFA1	Free fatty acid	A	Human	X-ray	5KW2	5KW2_refined	2.8	A	Intermediate	42	82	-	-	-	-	T4-Lysozyme	-	(3~{S})-3-cyclopropyl-3-[2-[1-[2-[2,2-dimethylpropyl-(6-methylpyridin-2-yl)carbamoyl]-5-methoxy-phenyl]piperidin-4-yl]-1-benzofuran-6-yl]propanoic acid	small-molecule	Allosteric agonist	docosahexaenoic acid, oleic acid, α-linolenic acid, myristic acid	small-molecule	No	No	Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C	10.1038/S41467-017-01240-W	2018-05-02	Yes
C5AR1	C5a₁	Complement peptide	A	Human	X-ray	6C1Q	6C1Q_refined	2.9	B	Inactive	6	82	-	-	-	-	BRIL	-	PMX53 NDT9513727	peptide small-molecule	Antagonist NAM	C3a, C5a, C5a des-Arg, ribosomal protein S19	peptide	Yes	No	Liu H, Kim HR, Deepak RNVK, Wang L, Chung KY, Fan H, Wei Z, Zhang C	10.1038/S41594-018-0067-Z	2018-05-30	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	6DDF	6DDF_refined	3.5	R	Active	100	71	Gi/o	αi1	-	61	-	-	DAMGO	peptide	Agonist	-	-	Yes	No	Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK	10.1038/S41586-018-0219-7	2018-06-13	Yes
OPSD	Rhodopsin	Opsins	A	Human	cryo-EM	6CMO	6CMO_refined	4.5	R	Active	77	92	Gi/o	αi1	-	100	BRIL	Fab	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE	10.1038/S41586-018-0215-Y	2018-06-20	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	X-ray	6DRY	6DRY_refined	2.9	A	Intermediate	42	60	-	-	-	-	BRIL	-	methylergonovine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL	10.1038/s41594-018-0116-7	2018-08-29	Yes
PD2R2	DP₂	Prostanoid	A	Human	X-ray	6D26	6D26_refined	2.8	A	Inactive	24	82	-	-	-	-	T4-Lysozyme	-	fevipiprant	small-molecule	Antagonist	PGJ₂, PGD₂, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Wang L, Yao D, Deepak RNVK, Liu H, Xiao Q, Fan H, Gong W, Wei Z, Zhang C	10.1016/J.MOLCEL.2018.08.009	2018-10-03	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6H7L	6H7L_refined	2.7	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb6B9	Dobutamine	small-molecule	Agonist	-	-	Yes	No	Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG	10.1126/SCIENCE.AAU5595	2018-10-17	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	X-ray	6H7O	6H7O_refined	2.8	A	Active	100	60	-	-	-	-	Thioredoxin 1	Camelid antibody fragment Nb6B9	(S)-Cyanopindolol	small-molecule	Agonist	-	-	Yes	No	Warne T, Edwards PC, Dore AS, Leslie AGW, Tate CG	10.1126/SCIENCE.AAU5595	2018-10-17	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6MXT	6MXT_refined	3.0	A	Active	99	69	-	-	-	-	T4-Lysozyme	Nanobody-71	salmeterol	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, Kobilka BK	10.1038/s41589-018-0145-x	2018-11-14	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	X-ray	5ZKC	5ZKC_refined	2.3	A	Inactive	3	60	-	-	-	-	BRIL	-	N-methyl scopolamine	small-molecule	Antagonist	acetylcholine	small-molecule	No	No	Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T	10.1038/S41589-018-0152-Y	2018-11-21	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Rat	X-ray	5ZHP	5ZHP_refined	3.1	B	Inactive	3	47	-	-	-	-	T4-Lysozyme	-	(1R,2R,4S,5S,7s)-7-({[4-fluoro-2-(thiophen-2-yl)phenyl]carbamoyl}oxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0~2,4~]nonan-9-ium	small-molecule	Antagonist	acetylcholine	small-molecule	No	No	Liu H, Hofmann J, Fish I, Schaake B, Eitel K, Bartuschat A, Kaindl J, Rampp H, Banerjee A, Hubner H, Clark MJ, Vincent SG, Fisher JT, Heinrich MR, Hirata K, Liu X, Sunahara RK, Shoichet BK, Kobilka BK, Gmeiner P	10.1073/PNAS.1813988115	2018-11-28	Yes
PE2R4	EP₄	Prostanoid	A	Human	X-ray	5YHL	5YHL_refined	4.2	A	Inactive	11	57	-	-	-	-	-	Fab	ONO-AE3-208-Br	small-molecule	Antagonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	No	No	Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T	10.1038/S41589-018-0131-3	2018-12-05	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6E59	6E59_refined	3.4	A	Inactive	1	70	-	-	-	-	GlgA glycogen synthase	-	L760735	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Yin J, Chapman K, Clark LD, Shao Z, Borek D, Xu Q, Wang J, Rosenbaum DM	10.1073/PNAS.1812717115	2018-12-12	Yes
TA2R	TP	Prostanoid	A	Human	X-ray	6IIV	6IIV_refined	3.0	A	Intermediate	42	87	-	-	-	-	Rubredoxin	-	daltroban	small-molecule	Antagonist	PGD₂, thromboxane A₂, PGE₂, PGF_2α, PGI₂, PGH₂	small-molecule	No	No	Fan H, Chen S, Yuan X, Han S, Zhang H, Xia W, Xu Y, Zhao Q, Wu B	10.1038/S41589-018-0170-9	2018-12-19	Yes
CCR2	CCR2	Chemokine	A	Human	X-ray	6GPX	6GPX_refined	2.7	B	Inactive	16	70	-	-	-	-	Rubredoxin	-	MK-0812	small-molecule	Antagonist	CCL24, CCL2, CCL26, CCL8, CCL13, CCL7, CCL16, CCL11	peptide	No	No	Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G	10.1016/J.STR.2018.10.027	2019-01-02	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6HLL	6HLL_refined	3.3	A	Inactive	1	67	-	-	-	-	GlgA glycogen synthase	-	CP 99994	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A	10.1038/S41467-018-07939-8	2019-01-16	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6HLP	6HLP_refined	2.2	A	Inactive	1	71	-	-	-	-	GlgA glycogen synthase	-	netupitant	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Schoppe J, Ehrenmann J, Klenk C, Rucktooa P, Schutz M, Dore AS, Pluckthun A	10.1038/S41467-018-07939-8	2019-01-16	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	cryo-EM	6N52	6N52_refined	4.0	A	Inactive	-	64	-	-	-	-	-	Nanobody-43	-	-	-	L-glutamic acid	small-molecule	No	No	Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK	10.1038/S41586-019-0881-4	2019-01-23	Yes
CNR2	CB₂	Cannabinoid	A	Human	X-ray	5ZTY	5ZTY_refined	2.8	A	Inactive	9	80	-	-	-	-	T4-Lysozyme	-	AM10257	small-molecule	Antagonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Li X, Hua T, Vemuri K, Ho JH, Wu Y, Wu L, Popov P, Benchama O, Zvonok N, Locke K, Qu L, Han GW, Iyer MR, Cinar R, Coffey NJ, Wang J, Wu M, Katritch V, Zhao S, Kunos G, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ	10.1016/J.CELL.2018.12.011	2019-01-30	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	6DO1	6DO1_refined	2.9	A	Active	94	85	-	-	-	-	BRIL	Nanobody-Nb.AT110i1	CHEMBL404594	protein	Agonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Wingler LM, McMahon C, Staus DP, Lefkowitz RJ, Kruse AC	10.1016/J.CELL.2018.12.006	2019-01-30	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	6A93	6A93_refined	3.0	A	Inactive	1	60	-	-	-	-	BRIL	-	risperidone	small-molecule	Antagonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Kimura KT, Asada H, Inoue A, Kadji FMN, Im D, Mori C, Arakawa T, Hirata K, Nomura Y, Nomura N, Aoki J, Iwata S, Shimamura T	10.1038/S41594-018-0180-Z	2019-02-13	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	6A94	6A94_refined	2.9	A	Inactive	1	60	-	-	-	-	BRIL	-	zotepine	small-molecule	Antagonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Kimura KT, Asada H, Inoue A, Kadji FMN, Im D, Mori C, Arakawa T, Hirata K, Nomura Y, Nomura N, Aoki J, Iwata S, Shimamura T	10.1038/S41594-018-0180-Z	2019-02-13	Yes
NK1R	NK₁	Tachykinin	A	Human	X-ray	6J21	6J21_refined	3.2	A	Inactive	1	71	-	-	-	-	T4-Lysozyme	-	aprepitant	small-molecule	Antagonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Chen S, Lu M, Liu D, Yang L, Yi C, Ma L, Zhang H, Liu Q, Frimurer TM, Wang MW, Schwartz TW, Stevens RC, Wu B, Wuthrich K, Zhao Q	10.1038/S41467-019-08568-5	2019-03-06	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	6NBH	-	3.5	R	Active	100	64	Gs	αs	-	57	-	Nanobody-35	Long-acting parathyroid hormone analog	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y	10.1126/SCIENCE.AAV7942	2019-04-17	Yes
MTR1A	MT₁	Melatonin	A	Human	X-ray	6ME2	6ME2_refined	2.8	A	Inactive	1	83	-	-	-	-	GlgA glycogen synthase	-	ramelteon	small-molecule	Agonist	melatonin	small-molecule	No	No	Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V	10.1038/S41586-019-1141-3	2019-04-24	Yes
MTR1A	MT₁	Melatonin	A	Human	X-ray	6ME3	6ME3_refined	2.9	A	Inactive	1	82	-	-	-	-	GlgA glycogen synthase	-	2-phenylmelatonin	small-molecule	Agonist	melatonin	small-molecule	No	No	Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V	10.1038/S41586-019-1141-3	2019-04-24	Yes
MTR1A	MT₁	Melatonin	A	Human	X-ray	6ME4	6ME4_refined	3.2	A	Inactive	1	83	-	-	-	-	GlgA glycogen synthase	-	2-iodo-melatonin	small-molecule	Agonist	melatonin	small-molecule	No	No	Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V	10.1038/S41586-019-1141-3	2019-04-24	Yes
MTR1B	MT₂	Melatonin	A	Human	X-ray	6ME6	6ME6_refined	2.8	B	Inactive	1	78	-	-	-	-	Rubredoxin	-	2-phenylmelatonin	small-molecule	Agonist	melatonin	small-molecule	No	No	Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V	10.1038/S41586-019-1144-0	2019-04-24	Yes
MTR1B	MT₂	Melatonin	A	Human	X-ray	6ME8	6ME8_refined	3.1	B	Inactive	1	78	-	-	-	-	Rubredoxin	-	2-phenylmelatonin	small-molecule	Agonist	melatonin	small-molecule	Yes	No	Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V	10.1038/S41586-019-1144-0	2019-04-24	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6MH8	6MH8_refined	4.2	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Martin-Garcia JM, Zhu L, Mendez D, Lee MY, Chun E, Li C, Hu H, Subramanian G, Kissick D, Ogata C, Henning R, Ishchenko A, Dobson Z, Zhang S, Weierstall U, Spence JCH, Fromme P, Zatsepin NA, Fischetti RF, Cherezov V, Liu W	10.1107/S205225251900263X	2019-04-24	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	cryo-EM	6OIK	6OIK_refined	3.6	R	Active	100	60	Gi/o	αo	-	61	-	-	iperoxo LY2119620	small-molecule small-molecule	Agonist PAM	acetylcholine	small-molecule	Yes	No	Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK	10.1126/SCIENCE.AAW5188	2019-05-08	Yes
SMO	SMO	Frizzled	F	Human	cryo-EM	6OT0	-	3.9	R	Active	100	46	Gi/o	αi1	-	100	-	Fab light chain Fab heavy chain	24,25-Epoxy-cholesterol	small-molecule	Agonist	-	-	No	No	Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X	10.1038/S41586-019-1286-0	2019-06-12	Yes
B1B1U5	Rhodopsin	Opsins	A	Hasarius adansoni	X-ray	6I9K	-	2.2	A	Inactive	16	83	-	-	-	-	-	-	Retinal (11-cis)	small-molecule	Inverse agonist	-	-	Yes	No	Varma N, Mutt E, Muhle J, Panneels V, Terakita A, Deupi X, Nogly P, Schertler GFX, Lesca E	10.1073/PNAS.1902192116	2019-07-03	Yes
NTR1	NTS₁	Neurotensin	A	Human	cryo-EM	6OS9	6OS9_refined	3.0	R	Active	100	73	Gi/o	αi1	-	62	-	scFv16	JMV449	peptide	Agonist	large neuromedin N, neurotensin, neuromedin N, large neurotensin	peptide	Yes	No	Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G	10.1038/S41586-019-1337-6	2019-07-10	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	6QNO	6QNO_refined	4.4	R	Active	100	96	Gi/o	αi1	-	60	-	Fab antibody fragment light chain Fab antibody fragment heavy chain	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G	10.7554/ELIFE.46041	2019-07-10	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	6OY9	6OY9_refined	3.9	R	Active	100	94	Gi/o	αt1	-	64	-	-	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G	10.1016/J.MOLCEL.2019.06.007	2019-07-24	Yes
SUCR1	succinate	Succinate	A	Rat	X-ray	6IBB	6IBB_refined	2.1	A	Intermediate	42	93	-	-	-	-	-	Nanobody-6	-	-	-	-	-	Yes	No	Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP	10.1038/S41586-019-1663-8	2019-08-14	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	6OFJ	6OFJ_refined	4.5	A	Inactive	22	93	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhao DY, Poge M, Morizumi T, Gulati S, Van Eps N, Zhang J, Miszta P, Filipek S, Mahamid J, Plitzko JM, Baumeister W, Ernst OP, Palczewski K	10.1074/JBC.RA119.010089	2019-08-21	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	6KQI	6KQI_refined	3.3	A	Inactive	9	60	-	-	-	-	GlgA glycogen synthase	-	CP55940 Org27569	small-molecule small-molecule	Agonist NAM	anandamide, 2-arachidonoylglycerol	small-molecule	No	No	Shao Z, Yan W, Chapman K, Ramesh K, Ferrell AJ, Yin J, Wang X, Xu Q, Rosenbaum DM	10.1038/S41589-019-0387-2	2019-10-23	Yes
CLTR1	CysLT₁	Leukotriene	A	Human	X-ray	6RZ4	6RZ4_refined	2.7	A	Intermediate	42	85	-	-	-	-	BRIL	-	pranlukast	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	Yes	Yes	Luginina A, Gusach A, Marin E, Mishin A, Brouillette R, Popov P, Shiriaeva A, Besserer-Offroy E, Longpre JM, Lyapina E, Ishchenko A, Patel N, Polovinkin V, Safronova N, Bogorodskiy A, Edelweiss E, Hu H, Weierstall U, Liu W, Batyuk A, Gordeliy V, Han GW, Sarret P, Katritch V, Borshchevskiy V, Cherezov V	10.1126/SCIADV.AAX2518	2019-10-30	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	6KJV	6KJV_refined	2.8	B	Inactive	0	57	-	-	-	-	T4-Lysozyme	-	PF-06372222	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G	10.1107/S2052252519013496	2019-11-13	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	6KK7	6KK7_refined	3.1	B	Inactive	0	56	-	-	-	-	T4-Lysozyme	-	PF-06372222	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Xu Y, Wang Y, Wang Y, Liu K, Peng Y, Yao D, Tao H, Liu H, Song G	10.1107/S2052252519013496	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS0	6PS0_refined	3.4	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	carazolol	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS2	6PS2_refined	2.4	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	CHEMBL1160734	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS4	6PS4_refined	2.6	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	CHEMBL1233766	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6PS6	6PS6_refined	2.7	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	timolol	small-molecule	Antagonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
MTR1A	MT₁	Melatonin	A	Human	X-ray	6PS8	6PS8_refined	3.3	A	Inactive	1	83	-	-	-	-	GlgA glycogen synthase	-	2-phenylmelatonin	small-molecule	Agonist	melatonin	small-molecule	No	No	Ishchenko A, Stauch B, Han GW, Batyuk A, Shiriaeva A, Li C, Zatsepin N, Weierstall U, Liu W, Nango E, Nakane T, Tanaka R, Tono K, Joti Y, Iwata S, Moraes I, Gati C, Cherezov V	10.1107/S2052252519013137	2019-11-13	Yes
DRD4	D₄	Dopamine	A	Mouse	X-ray	6IQL	6IQL_refined	3.5	A	Inactive	14	65	-	-	-	-	BRIL	-	L745870	small-molecule	Antagonist	-	-	Yes	No	Zhou Y, Cao C, He L, Wang X, Zhang XC	10.7554/ELIFE.48822	2019-12-04	Yes
ADA2C	α_2C	Adrenoceptors	A	Human	X-ray	6KUW	6KUW_refined	2.8	A	Inactive	1	60	-	-	-	-	GlgA glycogen synthase	-	(8Ar,12aS,13aR)-12-ethylsulfonyl-3-methoxy-5,6,8,8a,9,10,11,12a,13,13a-decahydroisoquinolino[2,1-g][1,6]naphthyridine	small-molecule	Antagonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2019-12-04	Yes
NTR1	NTS₁	Neurotensin	A	Human	cryo-EM	6PWC	6PWC_refined	4.9	R	Active	100	77	Beta	Beta-arrestin-1	-	84	-	Fab30 heavy chain Fab30 light chain	CHEMBL48981	protein	Agonist	large neuromedin N, neurotensin, neuromedin N, large neurotensin	peptide	Yes	No	Yin W, Li Z, Jin M, Yin YL, de Waal PW, Pal K, Yin Y, Gao X, He Y, Gao J, Wang X, Zhang Y, Zhou H, Melcher K, Jiang Y, Cong Y, Edward Zhou X, Yu X, Eric Xu H	10.1038/S41422-019-0256-2	2019-12-04	Yes
OPRD	δ	Opioid	A	Human	X-ray	6PT2	6PT2_refined	2.8	A	Active	74	78	-	-	-	-	BRIL	-	KGCHM07	peptide	Agonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	No	No	Claff T, Yu J, Blais V, Patel N, Martin C, Wu L, Han GW, Holleran BJ, Van der Poorten O, White KL, Hanson MA, Sarret P, Gendron L, Cherezov V, Katritch V, Ballet S, Liu ZJ, Muller CE, Stevens RC	10.1126/SCIADV.AAX9115	2019-12-11	Yes
CLTR2	CysLT₂	Leukotriene	A	Human	X-ray	6RZ7	6RZ7_refined	2.4	A	Intermediate	42	79	-	-	-	-	BRIL	-	ONO-2570366	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	No	No	Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V	10.1038/S41467-019-13348-2	2019-12-11	Yes
CLTR2	CysLT₂	Leukotriene	A	Human	X-ray	6RZ9	6RZ9_refined	2.7	A	Intermediate	42	81	-	-	-	-	BRIL	-	ONO-2770372	small-molecule	Antagonist	LTC₄, LTE₄, LTD₄	small-molecule	No	No	Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V	10.1038/S41467-019-13348-2	2019-12-11	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TOD	-	2.1	A	Inactive	1	71	-	-	-	-	-	-	EMPA	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TP4	-	3.0	A	Inactive	1	70	-	-	-	-	-	-	ACT-462206	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	6TPG	6TPG_refined	2.7	A	Inactive	1	69	-	-	-	-	GlgA glycogen synthase	-	EMPA	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	6TPJ	6TPJ_refined	2.7	A	Inactive	1	68	-	-	-	-	GlgA glycogen synthase	-	suvorexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TQ6	6TQ6_refined	2.6	B	Inactive	1	71	-	-	-	-	-	-	CHEMBL4592653	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TQ9	6TQ9_refined	2.7	B	Inactive	1	71	-	-	-	-	-	-	SB-408124	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	6JOD	6JOD_refined	3.2	A	Active	100	84	-	-	-	-	BRIL	Heavy chain of 4A03Fab Light chain of 4A03Fab	angiotensin II	peptide	Agonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Asada H, Inoue A, Ngako Kadji FM, Hirata K, Shiimura Y, Im D, Shimamura T, Nomura N, Iwanari H, Hamakubo T, Kusano-Arai O, Hisano H, Uemura T, Suno C, Aoki J, Iwata S	10.1016/J.STR.2019.12.003	2020-01-15	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TOT	6TOT_refined	2.2	B	Inactive	1	71	-	-	-	-	-	-	lemborexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-15	Yes
APJ	apelin	Apelin	A	Human	X-ray	6KNM	6KNM_refined	3.2	B	Inactive	3	78	-	-	-	-	Rubredoxin	-	Single domain antibody JN241	protein	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Ma Y, Ding Y, Song X, Ma X, Li X, Zhang N, Song Y, Sun Y, Shen Y, Zhong W, Hu LA, Ma Y, Zhang MY	10.1126/SCIADV.AAX7379	2020-01-29	Yes
CNR2	CB₂	Cannabinoid	A	Human	X-ray	6KPC	6KPC_refined	3.2	A	Inactive	9	79	-	-	-	-	T4-Lysozyme	-	7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]-7-methyloctanenitrile	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ	10.1016/J.CELL.2020.01.008	2020-02-12	Yes
CNR1	CB₁	Cannabinoid	A	Human	cryo-EM	6KPG	6KPG_refined	3.0	R	Active	100	60	Gi/o	αi1	-	64	-	scFv16	AM841	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ	10.1016/J.CELL.2020.01.008	2020-02-12	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6NWE	6NWE_refined	2.7	A	Active	100	94	Gi/o	αt1	Only H5	3	-	-	B-Octylglucoside	small-molecule	unknown	-	-	No	No	-	-	2020-02-12	Yes
CRFR2	CRF₂	Corticotropin-releasing factor	B1	Human	cryo-EM	6PB1	6PB1_refined	2.8	P	Active	100	68	Gs	αs	-	58	-	Nanobody-35	Urocortin	peptide	Agonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2, urocortin 3	peptide	No	No	Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE	10.1016/J.MOLCEL.2020.01.013	2020-02-12	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	6OS0	6OS0_refined	2.9	A	Active	94	85	-	-	-	-	BRIL	Nanobody-Nb.AT110i1	angiotensin II	peptide	Agonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC	10.1126/SCIENCE.AAY9813	2020-02-19	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	6OS1	-	2.8	A	Active	94	85	-	-	-	-	BRIL	Nanobody-Nb.AT110i1_le	TRV023	peptide	Agonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC	10.1126/SCIENCE.AAY9813	2020-02-19	Yes
GPR52	GPR52	A orphans	A	Human	X-ray	6LI0	6LI0_refined	2.2	A	Inactive	38	81	-	-	-	-	Flavodoxin	-	derivative 17 [Nakahata et al., 2018]	small-molecule	Agonist	-	-	Yes	No	Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F	10.1038/S41586-020-2019-0	2020-02-26	Yes
GPR52	GPR52	A orphans	A	Human	cryo-EM	6LI3	6LI3_refined	3.3	R	Active	100	79	Gs	αs	Mini-Gs	61	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F	10.1038/S41586-020-2019-0	2020-02-26	Yes
ACM2	M₂	Acetylcholine (muscarinic)	A	Human	cryo-EM	6U1N	6U1N_refined	4.0	R	Active	100	57	Beta	Beta-arrestin-1	-	86	-	Fab30 light chain Fab30 heavy chain	LY2119620	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Staus DP, Hu H, Robertson MJ, Kleinhenz ALW, Wingler LM, Capel WD, Latorraca NR, Lefkowitz RJ, Skiniotis G	10.1038/S41586-020-1954-0	2020-02-26	Yes
NTR1	NTS₁	Neurotensin	A	Human	cryo-EM	6UP7	6UP7_refined	4.2	R	Active	100	77	Beta	Beta-arrestin-1	-	83	-	-	JMV431	peptide	Agonist	large neuromedin N, neurotensin, neuromedin N, large neurotensin	peptide	Yes	No	Huang W, Masureel M, Qu Q, Janetzko J, Inoue A, Kato HE, Robertson MJ, Nguyen KC, Glenn JS, Skiniotis G, Kobilka BK	10.1038/S41586-020-1953-1	2020-02-26	Yes
PACR	PAC₁	VIP and PACAP	B1	Human	cryo-EM	6LPB	6LPB_refined	3.9	R	Active	100	71	Gs	αs	-	57	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, PHI, PACAP-38, VIP, PHV	peptide	No	No	Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O	10.1038/S41594-020-0386-8	2020-03-11	Yes
PACR	PAC₁	VIP and PACAP	B1	Human	cryo-EM	6M1I	6M1I_refined	3.5	A	Active	100	75	Gs	αs	-	56	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, PHI, PACAP-38, VIP, PHV	peptide	No	No	Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y	10.1038/S41422-020-0280-2	2020-03-11	Yes
OPRK	κ	Opioid	A	Human	X-ray	6VI4	6VI4_refined	3.3	B	Inactive	3	73	-	-	-	-	-	Nanobody-6	JDTic	small-molecule	Antagonist	big dynorphin, β-neoendorphin, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Che T, English J, Krumm BE, Kim K, Pardon E, Olsen RHJ, Wang S, Zhang S, Diberto JF, Sciaky N, Carroll FI, Steyaert J, Wacker D, Roth BL	10.1038/S41467-020-14889-7	2020-03-18	Yes
ADRB2	β₂	Adrenoceptors	A	Human	X-ray	6OBA	6OBA_refined	3.1	A	Inactive	0	68	-	-	-	-	T4-Lysozyme	-	CHEMBL1160734 AS408	small-molecule small-molecule	Antagonist NAM	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	-	-	2020-03-25	Yes
GLR	glucagon	Glucagon	B1	Human	cryo-EM	6LMK	6LMK_refined	3.7	R	Active	100	83	Gs	αs	-	59	-	Nanobody-35	glucagon	peptide	Agonist	glucagon	peptide	No	No	Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B	10.1126/SCIENCE.AAZ5346	2020-04-01	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	6UUS	6UUS_refined	2.4	R	Active	100	74	Gs	αs	-	48	-	Nanobody-35 RAMP3	Adrenomedullin	peptide	Agonist	-	-	No	No	-	-	2020-04-01	Yes
ADA2B	α_2B	Adrenoceptors	A	Human	cryo-EM	6K41	-	2.9	R	Active	100	54	Gi/o	αo	-	60	T4-Lysozyme	scFv	dexmedetomidine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK	10.1038/S41589-020-0492-2	2020-04-15	Yes
ADA2B	α_2B	Adrenoceptors	A	Human	cryo-EM	6K42	-	4.1	R	Active	100	60	Gi/o	αi1	-	62	T4-Lysozyme	scFv	dexmedetomidine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK	10.1038/S41589-020-0492-2	2020-04-15	Yes
MC4R	MC₄	Melanocortin	A	Human	X-ray	6W25	-	2.8	A	Intermediate	46	79	-	-	-	-	GlgA glycogen synthase	-	SHU9119 Calcium	peptide small-molecule	Antagonist Cofactor	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	Yu J, Gimenez LE, Hernandez CC, Wu Y, Wein AH, Han GW, McClary K, Mittal SR, Burdsall K, Stauch B, Wu L, Stevens SN, Peisley A, Williams SY, Chen V, Millhauser GL, Zhao S, Cone RD, Stevens RC	10.1126/SCIENCE.AAZ8995	2020-04-29	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6UO8	-	3.6	B	Active	-	74	-	-	-	-	-	-	CHEMBL112710 GS39783	small-molecule small-molecule	Agonist PAM	-	-	No	No	Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V	10.1038/S41586-020-2408-4	2020-06-10	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6UO9	-	4.8	B	Intermediate	-	73	-	-	-	-	-	-	CHEMBL112710	small-molecule	Agonist	-	-	No	No	Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V	10.1038/S41586-020-2408-4	2020-06-10	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	6TKO	6TKO_refined	3.3	A	Active	100	58	Beta	Beta-arrestin-1	-	82	-	Fab30 heavy chain Fab30 light chain	arformoterol	small-molecule	Agonist	-	-	Yes	No	Lee Y, Warne T, Nehme R, Pandey S, Dwivedi-Agnihotri H, Chaturvedi M, Edwards PC, Garcia-Nafria J, Leslie AGW, Shukla AK, Tate CG	10.1038/S41586-020-2419-1	2020-06-17	Yes
DRD2	D₂	Dopamine	A	Human	cryo-EM	6VMS	6VMS_refined	3.8	R	Active	100	63	Gi/o	αi1	-	64	T4-Lysozyme	scFv16	bromocriptine	small-molecule	Agonist	dopamine	small-molecule	Yes	No	Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM	10.1038/S41586-020-2379-5	2020-06-17	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6PGS	6PGS_refined	2.9	A	Active	100	94	Gi/o	αt2	Only H5	3	-	-	Geraniol	small-molecule	unknown	-	-	No	No	-	-	2020-07-01	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6PH7	6PH7_refined	2.9	A	Active	100	94	Gi/o	αt2	Only H5	3	-	-	Nerol	small-molecule	unknown	-	-	No	No	-	-	2020-07-01	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6W2X	-	3.6	B	Inactive	-	71	-	-	-	-	-	-	CGP55845 1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine	small-molecule small-molecule	Inverse agonist NAM	-	-	No	No	Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G	10.1038/S41586-020-2469-4	2020-07-01	Yes
GABR1	GABA_B1	GABA_B	C	Human	cryo-EM	6W2Y	-	3.2	B	Inactive	-	69	-	-	-	-	-	-	CGP55845 1-Stearoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine	small-molecule small-molecule	Inverse agonist NAM	GABA	small-molecule	No	No	Papasergi-Scott MM, Robertson MJ, Seven AB, Panova O, Mathiesen JM, Skiniotis G	10.1038/S41586-020-2469-4	2020-07-01	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7C7S	-	2.9	B	Inactive	-	71	-	-	-	-	-	-	CGP 54626A	small-molecule	Antagonist	-	-	No	No	Mao C, Shen C, Li C, Shen DD, Xu C, Zhang S, Zhou R, Shen Q, Chen LN, Jiang Z, Liu J, Zhang Y	10.1038/S41422-020-0350-5	2020-07-01	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6VCB	6VCB_refined	3.3	R	Active	100	82	Gs	αs	-	57	-	Nanobody-35	glucagon-like peptide 1-(7-37) LSN3160440	peptide small-molecule	Agonist PAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW	10.1038/S41589-020-0589-7	2020-07-22	Yes
SCTR	secretin	Glucagon	B1	Human	cryo-EM	6WZG	6WZG_refined	2.3	R	Active	100	86	Gs	αs	-	61	-	Nanobody-35	SECRETIN	protein	Agonist	secretin, VIP	peptide	No	No	Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ	10.1038/S41467-020-17791-4	2020-08-12	Yes
CXCR2	CXCR2	Chemokine	A	Human	cryo-EM	6LFO	6LFO_refined	3.4	R	Active	100	85	Gi/o	αi1	-	65	-	scFv16	Interleukin-8	protein	Agonist	CXCL7, CXCL8, CXCL6, CXCL2, CXCL1, CXCL5, CXCL3	peptide	No	No	Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ	10.1038/S41586-020-2492-5	2020-09-02	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6X1A	6X1A_refined	2.5	R	Active	100	84	Gs	αs	-	89	-	Nanobody-35	danuglipron	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Singh N, Singh D, Bhide A, Sharma R, Bhowmick S, Patel V, Modi D	10.1101/2020.08.16.252585	2020-09-09	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6ZDV	6ZDV_refined	2.1	A	Inactive	1	72	-	-	-	-	BRIL	-	2-Methyl-3-(4-methylthiazol-2-yl)-4-oxo-6-propyl-4H-chromen-7-yl acetate	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Jespers W, Verdon G, Azuaje J, Majellaro M, Keranen H, Garcia-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Dore AS, Mason JS, Aqvist J, Cooke RM, Sotelo E, Gutierrez-de-Teran H	10.1002/ANIE.202003788	2020-09-16	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	cryo-EM	6WHA	6WHA_refined	3.4	A	Active	100	52	Gq/11	αq	Gq-Gi2-Gs chimera	59	BRIL	scFv16	25-CN-NBOH	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	Yes	No	Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL	10.1016/J.CELL.2020.08.024	2020-09-23	Yes
SMO	SMO	Frizzled	F	Human	cryo-EM	6XBK	6XBK_refined	3.2	R	Active	100	59	Gi/o	αi1	-	61	-	scFv16	Cholesterol	small-molecule	Agonist	-	-	No	No	Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X	10.1038/S41589-020-0646-2	2020-09-30	Yes
GNRHR	GnRH₁	Gonadotrophin-releasing hormone	A	Human	X-ray	7BR3	7BR3_refined	2.8	A	Inactive	34	84	-	-	-	-	GlgA glycogen synthase	-	elagolix	small-molecule	Antagonist	GnRH II, GnRH I	peptide	No	No	-	-	2020-10-07	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7CA3	-	4.5	B	Active	-	72	-	-	-	-	-	-	BHFF	small-molecule	PAM	-	-	No	No	Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y	10.1016/J.JMB.2020.09.023	2020-11-11	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7CA5	-	7.6	B	Inactive	-	70	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y	10.1016/J.JMB.2020.09.023	2020-11-11	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6WQA	6WQA_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Lee MY, Geiger J, Ishchenko A, Han GW, Barty A, White TA, Gati C, Batyuk A, Hunter MS, Aquila A, Boutet S, Weierstall U, Cherezov V, Liu W	10.1107/S2052252520012701	2020-11-18	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6XOX	6XOX_refined	3.1	R	Active	100	82	Gs	αs	-	56	-	scFv16 Nanobody-35	LY3502970	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	-	-	2020-11-18	Yes
GHRHR	GHRH	Glucagon	B1	Human	cryo-EM	7CZ5	7CZ5_refined	2.6	R	Active	100	64	Gs	αs	-	58	-	Nanobody-35	Somatoliberin	peptide	Agonist	GHRH	peptide	No	No	Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW	10.1038/S41467-020-18945-0	2020-11-18	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6LPK	6LPK_refined	1.8	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M	10.1038/S41598-020-76277-X	2020-11-25	Yes
ADRB1	β₁	Adrenoceptors	A	Human	X-ray	7BTS	7BTS_refined	3.1	A	Active	100	58	-	-	-	-	T4-Lysozyme	Camelid antibody fragment Nb6B9	(-)-adrenaline	small-molecule	Agonist	noradrenaline, L-NOREPINEPHRINE, (-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X	10.1038/S41422-020-00424-2	2020-12-02	Yes
ADRB1	β₁	Adrenoceptors	A	Human	X-ray	7BU7	7BU7_refined	2.6	A	Active	100	58	-	-	-	-	T4-Lysozyme	Camelid antibody fragment Nb6B9	CHEMBL1615159	small-molecule	Agonist	noradrenaline, L-NOREPINEPHRINE, (-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X	10.1038/S41422-020-00424-2	2020-12-02	Yes
STE2	STE2	STE2	D1	strain ATCC 204508 / S288c	cryo-EM	7AD3	-	3.5	A	Active	-	69	GPa1 family	αPa1	Two alpha subunits bound to STE2 dimer	46	-	-	Alpha-factor mating pheromone	peptide	Agonist	-	-	No	No	Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG	10.1038/S41586-020-2994-1	2020-12-09	Yes
ADRB2	β₂	Adrenoceptors	A	Human	cryo-EM	7DHI	7DHI_refined	3.3	R	Active	100	70	Gs	αs	-	55	-	Nanobody-35	levosalbutamol	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Deng X, Li N, Mguni D, Wang J, Yang Y	10.1093/NSR/NWAA284	2020-12-16	Yes
DRD2	D₂	Dopamine	A	Human	X-ray	7DFP	7DFP_refined	3.1	A	Inactive	1	57	-	-	-	-	BRIL	Fab heavy chain Fab light chain	spiperone	small-molecule	Antagonist	dopamine	small-molecule	No	No	Im D, Inoue A, Fujiwara T, Nakane T, Yamanaka Y, Uemura T, Mori C, Shiimura Y, Kimura KT, Asada H, Nomura N, Tanaka T, Yamashita A, Nango E, Tono K, Kadji FMN, Aoki J, Iwata S, Shimamura T	10.1038/S41467-020-20221-0	2020-12-30	Yes
NTR1	NTS₁	Neurotensin	A	Rat	cryo-EM	7L0Q	7L0Q_refined	4.3	C	Active	100	73	Gi/o	αi1	-	95	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	-	-	2021-01-06	Yes
NTR1	NTS₁	Neurotensin	A	Rat	cryo-EM	7L0S	7L0S_refined	4.5	C	Active	100	73	Gi/o	αi1	Non-canonical conformation	95	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	-	-	2021-01-06	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7LCJ	7LCJ_refined	2.8	R	Active	98	84	-	-	-	-	-	-	danuglipron	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	-	-	2021-01-20	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7LCK	7LCK_refined	3.2	R	Active	98	84	-	-	-	-	-	-	danuglipron	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	-	-	2021-01-20	Yes
AGRG3	ADGRG3	ADGRG	B2	Human	cryo-EM	7D76	-	3.1	R	Active	100	48	Gi/o	αo	-	59	-	-	Beclomethasone	small-molecule	Agonist	-	-	No	No	Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP	10.1038/S41586-020-03083-W	2021-02-03	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6YVR	-	2.5	B	Inactive	2	83	-	-	-	-	DARPin D12	-	JMV431	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6Z66	-	3.2	A	Intermediate	14	80	-	-	-	-	DARPin D12	-	Apo (no ligand)	none	Apo (no ligand)	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6Z8N	-	2.8	A	Intermediate	14	80	-	-	-	-	DARPin D12	-	(2~{S})-4-methyl-2-[(1-quinolin-8-ylsulfonylindol-3-yl)carbonylamino]pentanoic acid	small-molecule	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6ZIN	-	2.6	A	Inactive	27	76	-	-	-	-	DARPin D12	-	meclinertant	small-molecule	Inverse agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
OX2R	OX₂	Orexin	A	Human	cryo-EM	7L1V	7L1V_refined	3.0	R	Active	100	64	Gs	αs	Engineered G alpha	58	-	scFv16 Nanobody-51	compound 1 [PMID: 33547286]	small-molecule	Agonist	orexin-A, orexin-B	peptide	Yes	No	Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K	10.1038/S41467-021-21087-6	2021-02-10	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7JV5	7JV5_refined	3.0	R	Active	100	63	Gs	αs	-	60	-	Nanobody-35	CHEMBL1160787	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE	10.1016/J.CELL.2021.01.027	2021-02-24	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7JVQ	7JVQ_refined	3.0	R	Active	100	64	Gs	αs	Engineered G alpha	60	-	Nanobody-35	apomorphine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE	10.1016/J.CELL.2021.01.027	2021-02-24	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	7KNT	7KNT_refined	3.2	R	Inactive	8	74	-	-	-	-	-	RAMP1	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Josephs TM, Belousoff MJ, Liang YL, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM	10.1126/SCIENCE.ABF7258	2021-02-24	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	7KNU	7KNU_refined	3.5	R	Inactive	8	74	-	-	-	-	-	RAMP1	Calcitonin gene-related peptide 1	peptide	Agonist	-	-	No	No	Josephs TM, Belousoff MJ, Liang YL, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM	10.1126/SCIENCE.ABF7258	2021-02-24	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7CKX	7CKX_refined	3.5	R	Active	100	61	Gs	αs	-	60	-	Nanobody-35	A77636	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z	10.1016/J.CELL.2021.01.028	2021-03-03	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7CKZ	7CKZ_refined	3.1	R	Active	100	62	Gs	αs	-	60	-	Nanobody-35	dopamine LY3154207	small-molecule small-molecule	Agonist PAM	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z	10.1016/J.CELL.2021.01.028	2021-03-03	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7LJC	-	3.0	R	Active	100	63	Gs	αs	Engineered G alpha	58	-	Nanobody-35	CHEMBL1160787 LY3154207	small-molecule small-molecule	Agonist PAM	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Singh N, Singh D, Bhide A, Sharma R, Bhowmick S, Patel V, Modi D	10.1101/2021.02.07.430101	2021-03-03	Yes
DRD3	D₃	Dopamine	A	Human	cryo-EM	7CMU	7CMU_refined	3.0	R	Active	100	68	Gi/o	αi1	-	64	BRIL	scFv16	pramipexole	small-molecule	Agonist	dopamine	small-molecule	Yes	No	Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE	10.1016/J.MOLCEL.2021.01.003	2021-03-10	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DTT	7DTT_refined	3.8	A	Active	-	72	-	-	-	-	-	-	Calcium	small-molecule	Agonist	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C	10.1038/S41422-021-00474-0	2021-03-10	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DTV	7DTV_refined	3.5	A	Active	-	72	-	-	-	-	-	-	Calcium L-tryptophan	small-molecule small-molecule	Agonist PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C	10.1038/S41422-021-00474-0	2021-03-10	Yes
HRH1	H₁	Histamine	A	Human	cryo-EM	7DFL	7DFL_refined	3.3	R	Active	100	56	Gq/11	αq	-	63	-	scFv16	histamine	small-molecule	Agonist	histamine	small-molecule	Yes	No	-	-	2021-03-31	Yes
5HT1A	5-HT_1A	5-Hydroxytryptamine	A	Human	cryo-EM	7E2Y	7E2Y_refined	3.0	R	Active	100	65	Gi/o	αi1	-	62	-	-	5-hydroxytryptamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE	10.1038/S41586-021-03376-8	2021-04-14	Yes
5HT1E	5-HT_1E	5-Hydroxytryptamine	A	Human	cryo-EM	7E33	7E33_refined	2.9	R	Active	100	70	Gi/o	αi1	-	61	-	scFv16	BRL-54443	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	Yes	No	Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE	10.1038/S41586-021-03376-8	2021-04-14	Yes
5HT1D	5-HT_1D	5-Hydroxytryptamine	A	Human	cryo-EM	7E32	7E32_refined	2.9	R	Active	100	76	Gi/o	αi1	-	62	-	scFv16	5-hydroxytryptamine	small-molecule	Agonist	5-HT-moduline, 5-hydroxytryptamine	small-molecule	Yes	No	Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE	10.1038/S41586-021-03376-8	2021-04-21	Yes
PE2R2	EP₂	Prostanoid	A	Human	cryo-EM	7CX2	7CX2_refined	2.8	R	Active	100	74	Gs	αs	-	58	-	Nanobody-35	PGE₂	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y	10.1126/SCIADV.ABF1268	2021-05-05	Yes
PE2R2	EP₂	Prostanoid	A	Human	cryo-EM	7CX4	7CX4_refined	2.9	R	Active	100	74	Gs	αs	-	58	-	Nanobody-35	evatanepag	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y	10.1126/SCIADV.ABF1268	2021-05-05	Yes
V2R	V₂	Vasopressin and oxytocin	A	Human	cryo-EM	7KH0	7KH0_refined	2.8	R	Active	100	74	Gs	αs	-	58	-	scFv16 Nanobody-35	vasopressin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C	10.1038/S41422-021-00483-Z	2021-05-26	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7MBX	7MBX_refined	2.0	R	Active	100	68	Gs	αs	-	61	-	Nanobody-35	CHEMBL216166	protein	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	-	-	2021-05-26	Yes
V2R	V₂	Vasopressin and oxytocin	A	Human	cryo-EM	7BB6	7BB6_refined	4.2	A	Active	100	73	Gs	αs	-	54	-	Nanobody-35	vasopressin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B	10.1126/SCIADV.ABG5628	2021-06-02	Yes
S1PR3	S1P₃	Lysophospholipid (S1P)	A	Human	X-ray	7C4S	7C4S_refined	3.2	A	Active	82	75	-	-	-	-	-	Fab light chain Fab heavy chain	sphingosine 1-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Maeda S, Shiimura Y, Asada H, Hirata K, Luo F, Nango E, Tanaka N, Toyomoto M, Inoue A, Aoki J, Iwata S, Hagiwara M	10.1126/SCIADV.ABF5325	2021-06-09	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DD6	-	3.2	B	Active	-	73	-	-	-	-	-	-	Calcium L-tryptophan	small-molecule small-molecule	Agonist PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X	10.1126/SCIADV.ABG1483	2021-06-16	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DD7	-	3.2	B	Active	-	73	-	-	-	-	-	-	Calcium L-tryptophan evocalcet	small-molecule small-molecule small-molecule	Agonist PAM PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X	10.1126/SCIADV.ABG1483	2021-06-16	Yes
GRM4	mGlu₄	Metabotropic glutamate	C	Human	cryo-EM	7E9H	7E9H_refined	4.0	R	Intermediate	-	84	Gi/o	αi3	-	63	-	scFv16	L-serine-O-phosphate	small-molecule	Agonist	L-serine-O-phosphate, L-glutamic acid	small-molecule	No	No	Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B	10.1038/S41586-021-03495-2	2021-06-23	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7EPB	7EPB_refined	3.1	B	Active	-	89	-	-	-	-	-	Anti-RON nanobody	eglumegad	small-molecule	Agonist	L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7EPD	7EPD_refined	3.9	A	Inactive	-	89	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	X-ray	7EPF	7EPF_refined	2.7	A	Inactive	-	28	-	-	-	-	Flavodoxin	-	(8~{R})-4-[2,4-Bis(fluoranyl)phenyl]-8-methyl-7-[(2-methylpyrazol-3-yl)methyl]-6,8-dihydro-5~{H}-1,7-naphthyridine-2-carboxamide	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7M3F	7M3F_refined	2.8	B	Active	-	75	-	-	-	-	-	-	Calcium L-tryptophan cinacalcet	small-molecule small-molecule small-molecule	Agonist PAM PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03691-0	2021-06-30	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7M3J	7M3J_refined	4.1	A	Inactive	-	72	-	-	-	-	-	-	NPS 2143	small-molecule	NAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03691-0	2021-06-30	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	7O7F	7O7F_refined	3.2	C	Active	100	85	Gi/o	αi1	-	62	-	Fab heavy chain Fab light chain	CCL5	peptide	Agonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S	10.1126/SCIADV.ABG8685	2021-06-30	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	7MTA	7MTA_refined	4.1	R	Active	97	93	-	-	-	-	-	Fab heavy chain Fab light chain GRK1	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Chen Q, Plasencia M, Li Z, Mukherjee S, Patra D, Chen CL, Klose T, Yao XQ, Kossiakoff AA, Chang L, Andrews PC, Tesmer JJG	10.1038/S41586-021-03721-X	2021-07-07	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7MTQ	-	3.7	B	Inactive	-	85	-	-	-	-	-	-	LY341495	small-molecule	Antagonist	L-glutamic acid	small-molecule	No	No	Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03680-3	2021-07-07	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7MTS	7MTS_refined	3.2	A	Active	-	90	Gi/o	αi1	-	58	-	-	2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine L-glutamic acid	small-molecule small-molecule	Ago-PAM Agonist	L-glutamic acid	small-molecule	No	No	Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03680-3	2021-07-07	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	7F1Q	7F1Q_refined	2.9	R	Active	100	84	Gi/o	αi1	-	61	-	-	CCL3	peptide	Agonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B	10.1038/S41467-021-24438-5	2021-07-14	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7E6T	7E6T_refined	3.0	A	Active	-	74	-	-	-	-	-	-	Calcium Cyclomethyltryptophan	small-molecule small-molecule	Agonist PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Chen X, Wang L, Cui Q, Ding Z, Han L, Kou Y, Zhang W, Wang H, Jia X, Dai M, Shi Z, Li Y, Li X, Geng Y	10.7554/ELIFE.68578	2021-09-22	Yes
S1PR5	S1P₅	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW1	7EW1_refined	3.4	A	Active	100	68	Gi/o	αi1	-	64	-	scFv16	siponimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z	10.1038/S41422-021-00566-X	2021-09-29	Yes
S1PR3	S1P₃	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW3	-	3.1	R	Active	100	77	Gi/o	αi1	-	64	-	scFv16	Sphingosine 1-phosphate	lipid	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z	10.1038/S41422-021-00567-W	2021-09-29	Yes
LSHR	LH	Glycoprotein hormone	A	Human	cryo-EM	7FIG	-	3.9	R	Active	100	79	Gs	αs	-	91	-	Nanobody-35	Choriogonadotropin beta Glycoprotein alpha	protein protein	Agonist	LH, hCG	peptide	Yes	No	Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE	10.1038/S41586-021-03924-2	2021-09-29	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TQ7	6TQ7_refined	2.7	A	Inactive	1	71	-	-	-	-	-	-	SB-334867	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-01	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6ORV	-	3.0	E	Active	100	61	Gs	αs	-	48	-	Nanobody-35	CHEMBL3950796	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D	10.1038/s41586-019-1902-z	2020-01-08	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6TOS	6TOS_refined	2.1	B	Inactive	1	72	-	-	-	-	-	-	CHEMBL2413522	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA.	10.1021/acs.jmedchem.9b01787	2020-01-15	Yes
CRFR1	CRF₁	Corticotropin-releasing factor	B1	Human	cryo-EM	6P9X	6P9X_refined	2.9	R	Active	100	65	Gs	αs	-	49	-	Nanobody-35	Corticoliberin	peptide	Agonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2	peptide	No	No	Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D	10.1016/J.MOLCEL.2020.01.012	2020-02-05	Yes
PACR	PAC₁	VIP and PACAP	B1	Human	cryo-EM	6P9Y	6P9Y_refined	3.0	R	Active	100	55	Gs	αs	-	49	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, PHI, PACAP-38, VIP, PHV	peptide	No	No	-	-	2020-02-05	Yes
CNR2	CB₂	Cannabinoid	A	Human	cryo-EM	6KPF	6KPF_refined	2.9	R	Active	100	81	Gi/o	αi1	-	62	-	scFv16	7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]-7-methyloctanenitrile	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ	10.1016/J.CELL.2020.01.008	2020-02-12	Yes
EDNRB	ET_B	Endothelin	A	Human	X-ray	6LRY	6LRY_refined	3.0	A	Inactive	14	70	-	-	-	-	T4-Lysozyme	-	sarafotoxin S6b	peptide	Agonist	endothelin-1, endothelin-2, endothelin-3	peptide	Yes	No	Izume T, Miyauchi H, Shihoya W, Nureki O	10.1016/J.BBRC.2019.12.091	2020-02-12	Yes
CRFR1	CRF₁	Corticotropin-releasing factor	B1	Human	cryo-EM	6PB0	6PB0_refined	3.0	R	Active	100	68	Gs	αs	Gs-Gi1 chimera	58	-	Nanobody-35	Urocortin	peptide	Agonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2	peptide	No	No	Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE	10.1016/J.MOLCEL.2020.01.013	2020-02-12	Yes
CNR2	CB₂	Cannabinoid	A	Human	cryo-EM	6PT0	6PT0_refined	3.2	R	Active	100	83	Gi/o	αi1	-	100	-	scFv16	WIN55212-2	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ	10.1016/J.CELL.2020.01.007	2020-02-12	Yes
AGTR1	AT₁	Angiotensin	A	Human	X-ray	6OS2	-	2.7	A	Active	94	85	-	-	-	-	BRIL	Nanobody-Nb.AT110i1_le	TRV026	peptide	Agonist	angiotensin A, angiotensin IV, angiotensin II, angiotensin III	peptide	Yes	No	Wingler LM, Skiba MA, McMahon C, Staus DP, Kleinhenz ALW, Suomivuori CM, Latorraca NR, Dror RO, Lefkowitz RJ, Kruse AC	10.1126/SCIENCE.AAY9813	2020-02-19	Yes
GPR52	GPR52	A orphans	A	Human	X-ray	6LI1	6LI1_refined	2.9	A	Inactive	38	81	-	-	-	-	Flavodoxin	-	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F	10.1038/S41586-020-2019-0	2020-02-26	Yes
GPR52	GPR52	A orphans	A	Human	X-ray	6LI2	6LI2_refined	2.8	A	Inactive	38	80	-	-	-	-	Rubredoxin	-	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F	10.1038/S41586-020-2019-0	2020-02-26	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	6OMM	6OMM_refined	3.2	R	Active	100	85	Gi/o	αi1	-	61	-	-	CHEMBL552527	protein	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C	10.1038/S41467-020-14728-9	2020-02-26	Yes
DRD2	D₂	Dopamine	A	Human	X-ray	6LUQ	6LUQ_refined	3.1	A	Inactive	1	59	-	-	-	-	T4-Lysozyme	-	haloperidol	small-molecule	Antagonist	dopamine	small-molecule	Yes	No	Fan L, Tan L, Chen Z, Qi J, Nie F, Luo Z, Cheng J, Wang S	10.1038/S41467-020-14884-Y	2020-03-04	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	X-ray	6KP6	6KP6_refined	3.0	A	Inactive	3	59	-	-	-	-	GlgA glycogen synthase	-	Apo (no ligand)	none	Apo (no ligand)	acetylcholine	small-molecule	Yes	No	Wang J, Wu M, Wu L, Xu Y, Li F, Wu Y, Popov P, Wang L, Bai F, Zhao S, Liu ZJ, Hua T	10.1107/S2052252520000597	2020-03-11	Yes
PACR	PAC₁	VIP and PACAP	B1	Human	cryo-EM	6M1H	6M1H_refined	3.6	A	Active	100	73	Gs	αs	-	54	-	Nanobody-35	maxadilan	peptide	Agonist	PACAP-27, PHM, PHI, PACAP-38, VIP, PHV	peptide	No	No	Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y	10.1038/S41422-020-0280-2	2020-03-11	Yes
GLP1R	GLP-1	Glucagon	B1	Human	X-ray	6LN2	6LN2_refined	3.2	A	Inactive	0	83	-	-	-	-	-	Fab7F38 light chain Fab7F38 heavy chain	PF-06372222	small-molecule	NAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Wu F, Yang L, Hang K, Laursen M, Wu L, Han GW, Ren Q, Roed NK, Lin G, Hanson MA, Jiang H, Wang MW, Reedtz-Runge S, Song G, Stevens RC	10.1038/S41467-020-14934-5	2020-03-18	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	X-ray	6LW5	6LW5_refined	2.8	A	Active	100	91	-	-	-	-	BRIL	-	CHEMBL552527	protein	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Chen T, Xiong M, Zong X, Ge Y, Zhang H, Wang M, Won Han G, Yi C, Ma L, Ye RD, Xu Y, Zhao Q, Wu B	10.1038/S41467-020-15009-1	2020-03-25	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	6UUN	6UUN_refined	3.0	R	Active	100	77	Gs	αs	-	48	-	Nanobody-35 RAMP2	Adrenomedullin	peptide	Agonist	-	-	No	No	-	-	2020-03-25	Yes
GLR	glucagon	Glucagon	B1	Human	cryo-EM	6LML	6LML_refined	3.9	R	Active	100	83	Gi/o	αi1	-	63	-	scFv16	glucagon	peptide	Agonist	glucagon	peptide	No	No	Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B	10.1126/SCIENCE.AAZ5346	2020-04-01	Yes
CALRL	calcitonin-like	Calcitonin	B1	Human	cryo-EM	6UVA	6UVA_refined	2.3	R	Active	100	75	Gs	αs	-	48	-	Nanobody-35 RAMP3	adrenomedullin 2/intermedin	peptide	Agonist	-	-	No	No	-	-	2020-04-01	Yes
GLR	glucagon	Glucagon	B1	Human	cryo-EM	6WHC	6WHC_refined	3.4	R	Active	100	78	Gs	αs	-	56	-	Nanobody-35	Dual-agonist peptide P15	peptide	Agonist	glucagon	peptide	No	No	Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM	10.1074/JBC.RA120.013793	2020-05-27	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6UOA	-	6.3	B	Intermediate	-	71	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V	10.1038/S41586-020-2408-4	2020-06-10	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6VJM	-	4.0	B	Inactive	-	73	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Shaye H, Ishchenko A, Lam JH, Han GW, Xue L, Rondard P, Pin JP, Katritch V, Gati C, Cherezov V	10.1038/S41586-020-2408-4	2020-06-10	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	X-ray	6PEL	6PEL_refined	3.2	A	Active	100	93	Gi/o	αt1	Only H5	3	-	-	Citronellol	small-molecule	unknown	-	-	No	No	-	-	2020-06-24	Yes
CCR6	CCR6	Chemokine	A	Human	cryo-EM	6WWZ	6WWZ_refined	3.3	R	Active	100	83	Gi/o	αo	-	59	-	scFv16	CCL20	peptide	Agonist	beta-defensin 4A, CCL20	peptide	No	No	Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H	10.1038/S41467-020-16820-6	2020-06-24	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	6WIV	-	3.3	B	Inactive	-	71	-	-	-	-	-	-	[(2R)-3-[(Z)-icos-11-enoyl]oxy-2-[(Z)-octadec-9-enoyl]oxypropyl] 2-(trimethylazaniumyl)ethylphosphate (2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate	small-molecule small-molecule	NAM	-	-	No	No	Park J, Fu Z, Frangaj A, Liu J, Mosyak L, Shen T, Slavkovich VN, Ray KM, Taura J, Cao B, Geng Y, Zuo H, Kou Y, Grassucci R, Chen S, Liu Z, Lin X, Williams JP, Rice WJ, Eng ET, Huang RK, Soni RK, Kloss B, Yu Z, Javitch JA, Hendrickson WA, Slesinger PA, Quick M, Graziano J, Yu H, Fiehn O, Clarke OB, Frank J, Fan QR	10.1038/S41586-020-2452-0	2020-07-01	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6S0L	6S0L_refined	2.7	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	-	-	2020-07-15	Yes
OX1R	OX₁	Orexin	A	Human	X-ray	6V9S	6V9S_refined	3.5	A	Inactive	1	72	-	-	-	-	GlgA glycogen synthase	-	JH112	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Hellmann J, Drabek M, Yin J, Gunera J, Proll T, Kraus F, Langmead CJ, Hubner H, Weikert D, Kolb P, Rosenbaum DM, Gmeiner P	10.1073/PNAS.2002704117	2020-07-15	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	7C6A	7C6A_refined	3.4	A	Active	99	77	-	-	-	-	BRIL	IgG heavy chain IgG light chain	CHEMBL404594	protein	Agonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI	10.1038/S41598-020-68355-X	2020-07-29	Yes
GHSR	ghrelin	Ghrelin	A	Human	X-ray	6KO5	6KO5_refined	3.3	A	Inactive	1	80	-	-	-	-	BRIL	Fab7881 heavy chain Fab7881 light chain	CHEMBL1956994	small-molecule	Antagonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	No	No	-	-	2020-08-12	Yes
FZD5	FZD₅	Frizzled	F	Human	cryo-EM	6WW2	6WW2_refined	3.7	R	Inactive	22	55	-	-	-	-	BRIL	anti-BRIL Fab heavy chain anti-BRIL Fab light chain anti-Fab Nanobody	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Tsutsumi N, Mukherjee S, Waghray D, Janda CY, Jude KM, Miao Y, Burg JS, Aduri NG, Kossiakoff AA, Gati C, Garcia KC	10.7554/ELIFE.58464	2020-08-19	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7C2E	7C2E_refined	4.2	R	Active	100	82	Gs	αs	-	48	-	Nanobody-35	2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE	10.1038/S41422-020-0384-8	2020-08-26	Yes
GPBAR	GPBA	Bile acid	A	Human	cryo-EM	7BW0	7BW0_refined	3.9	R	Active	100	85	Gs	αs	-	56	BRIL	Nanobody-35	-	-	-	lithocholic acid, chenodeoxycholic acid, cholic acid, deoxycholic acid	small-molecule	No	No	Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R	10.1038/S41392-020-00262-Z	2020-09-02	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	7JJO	7JJO_refined	2.6	R	Active	100	58	Gs	αs	-	51	-	Nanobody-35	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY	10.1016/J.MOLCEL.2020.08.001	2020-09-02	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	6X19	6X19_refined	2.1	R	Active	100	84	Gs	αs	-	89	-	Nanobody-35	CHU-128	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Singh N, Singh D, Bhide A, Sharma R, Bhowmick S, Patel V, Modi D	10.1101/2020.08.16.252585	2020-09-09	Yes
GPBAR	GPBA	Bile acid	A	Human	cryo-EM	7CFM	7CFM_refined	3.0	R	Active	100	83	Gs	αs	-	58	-	Nanobody-35	CHEMBL2331646	small-molecule	Agonist	lithocholic acid, chenodeoxycholic acid, cholic acid, deoxycholic acid	small-molecule	No	No	Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y	10.1038/S41586-020-2569-1	2020-09-09	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6ZDR	6ZDR_refined	1.9	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL2030687	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Jespers W, Verdon G, Azuaje J, Majellaro M, Keranen H, Garcia-Mera X, Congreve M, Deflorian F, de Graaf C, Zhukov A, Dore AS, Mason JS, Aqvist J, Cooke RM, Sotelo E, Gutierrez-de-Teran H	10.1002/ANIE.202003788	2020-09-16	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	6WH4	6WH4_refined	3.4	C	Inactive	1	59	-	-	-	-	BRIL	-	CHEMBL428892	small-molecule	Inverse agonist	tryptamine, 5-hydroxytryptamine	small-molecule	Yes	No	Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL	10.1016/J.CELL.2020.08.024	2020-09-23	Yes
SMO	SMO	Frizzled	F	Human	cryo-EM	6XBL	6XBL_refined	3.9	R	Active	100	59	Gi/o	αi1	-	61	-	scFv16	Cholesterol SAG1.3	small-molecule small-molecule	Agonist PAM	-	-	No	No	Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X	10.1038/S41589-020-0646-2	2020-09-30	Yes
SCTR	secretin	Glucagon	B1	Human	cryo-EM	7D3S	7D3S_refined	2.9	R	Active	100	60	Gs	αs	-	58	-	Nanobody-35	SECRETIN	protein	Agonist	secretin, VIP	peptide	No	No	Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O	10.1016/J.BBRC.2020.08.042	2020-11-04	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7CUM	-	3.5	B	Inactive	-	72	-	-	-	-	-	-	CGP 54626A Unknown ligand	small-molecule none	Antagonist NAM	-	-	No	No	Kim Y, Jeong E, Jeong JH, Kim Y, Cho Y	10.1016/J.JMB.2020.09.023	2020-11-11	Yes
PE2R4	EP₄	Prostanoid	A	Human	cryo-EM	7D7M	7D7M_refined	3.3	A	Active	100	58	Gs	αs	-	58	-	Nanobody-35	PGE₂	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	No	No	-	-	2020-11-18	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6LPJ	6LPJ_refined	1.8	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M	10.1038/S41598-020-76277-X	2020-11-25	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	6LPL	6LPL_refined	2.0	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Ihara K, Hato M, Nakane T, Yamashita K, Kimura-Someya T, Hosaka T, Ishizuka-Katsura Y, Tanaka R, Tanaka T, Sugahara M, Hirata K, Yamamoto M, Nureki O, Tono K, Nango E, Iwata S, Shirouzu M	10.1038/S41598-020-76277-X	2020-11-25	Yes
ADRB1	β₁	Adrenoceptors	A	Human	X-ray	7BU6	7BU6_refined	2.7	A	Active	100	58	-	-	-	-	T4-Lysozyme	Camelid antibody fragment Nb6B9	Noradrenaline	small-molecule	Agonist	noradrenaline, L-NOREPINEPHRINE, (-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X	10.1038/S41422-020-00424-2	2020-12-02	Yes
ADRB1	β₁	Adrenoceptors	A	Human	X-ray	7BVQ	7BVQ_refined	2.5	A	Inactive	0	60	-	-	-	-	T4-Lysozyme	-	Carazolol	small-molecule	Inverse agonist	noradrenaline, L-NOREPINEPHRINE, (-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X	10.1038/S41422-020-00424-2	2020-12-02	Yes
GLP2R	GLP-2	Glucagon	B1	Human	cryo-EM	7D68	7D68_refined	3.0	R	Active	100	53	Gs	αs	-	57	-	Nanobody-35	glucagon	peptide	Agonist	glucagon-like peptide 2-(3-33), glucagon-like peptide 2	peptide	No	No	Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW	10.1038/S41422-020-00442-0	2020-12-16	Yes
ADRB2	β₂	Adrenoceptors	A	Human	cryo-EM	7DHR	7DHR_refined	3.8	R	Active	100	69	Gs	αs	-	49	-	Nanobody-35	LEVISOPRENALINE	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, L-NOREPINEPHRINE, Zn²⁺, (-)-adrenaline	small-molecule	Yes	No	Deng X, Li N, Mguni D, Wang J, Yang Y	10.1093/NSR/NWAA284	2020-12-16	Yes
NTR1	NTS₁	Neurotensin	A	Rat	cryo-EM	7L0P	7L0P_refined	4.1	C	Active	100	73	Gi/o	αi1	-	63	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	-	-	2021-01-06	Yes
NTR1	NTS₁	Neurotensin	A	Rat	cryo-EM	7L0R	7L0R_refined	4.2	C	Active	100	73	Gi/o	αi1	Non-canonical conformation	63	-	-	neurotensin	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	-	-	2021-01-06	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7LCI	7LCI_refined	2.9	R	Active	100	85	Gs	αs	-	62	-	-	danuglipron	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	-	-	2021-01-20	Yes
NPY2R	Y₂	Neuropeptide Y	A	Human	X-ray	7DDZ	7DDZ_refined	2.8	A	Inactive	1	76	-	-	-	-	Flavodoxin	-	CHEMBL1823578	small-molecule	Antagonist	neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY, pancreatic polypeptide	peptide	Yes	No	-	-	2021-01-27	Yes
AGRG3	ADGRG3	ADGRG	B2	Human	cryo-EM	7D77	7D77_refined	2.9	R	Active	100	48	Gi/o	αo	-	61	-	scFv16	HYDROCORTISONE	small-molecule	Agonist	-	-	No	No	Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP	10.1038/S41586-020-03083-W	2021-02-03	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6Z4Q	-	2.9	A	Inactive	27	75	-	-	-	-	DARPin D12	-	SR142948A	small-molecule	Inverse agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6Z4S	-	2.7	A	Inactive	2	77	-	-	-	-	DARPin D12	-	meclinertant	small-molecule	Inverse agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6Z4V	-	2.6	A	Intermediate	14	79	-	-	-	-	DARPin D12	-	JMV431	peptide	Agonist	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
NTR1	NTS₁	Neurotensin	A	Rat	X-ray	6ZA8	-	2.7	A	Intermediate	14	78	-	-	-	-	DARPin D12	-	CHEMBL508044	small-molecule	Agonist (partial)	neurotensin, neuromedin N	peptide	Yes	No	Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PRE, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Pluckthun A	10.1126/sciadv.abe5504	2021-02-10	Yes
OX2R	OX₂	Orexin	A	Human	cryo-EM	7L1U	7L1U_refined	3.2	R	Active	100	63	Gs	αs	Engineered G alpha	58	-	scFv16	Orexin-A	peptide	Agonist	orexin-A, orexin-B	peptide	Yes	No	Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K	10.1038/S41467-021-21087-6	2021-02-10	Yes
LT4R1	BLT₁	Leukotriene	A	Human	X-ray	7K15	7K15_refined	2.9	A	Inactive	3	85	-	-	-	-	Flavodoxin	-	N-(tert-butylsulfonyl)-4-fluoro-2-{(3S,4R)-4-hydroxy-3-[(pyridin-2-yl)methyl]-3,4-dihydro-2H-1-benzopyran-7-yl}benzamide	small-molecule	Antagonist	LTB₄, 20-hydroxy-LTB₄, 12R-HETE	small-molecule	Yes	Yes	-	-	2021-02-17	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7JVP	7JVP_refined	2.9	R	Active	100	63	Gs	αs	-	60	-	Nanobody-35	39YLC3L0ZU	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE	10.1016/J.CELL.2021.01.027	2021-02-24	Yes
DRD2	D₂	Dopamine	A	Human	cryo-EM	7JVR	7JVR_refined	2.8	R	Active	100	61	Gi/o	αi1	-	63	-	scFv16	bromocriptine	small-molecule	Agonist	dopamine	small-molecule	Yes	No	Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE	10.1016/J.CELL.2021.01.027	2021-02-24	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7CKW	7CKW_refined	3.2	R	Active	100	61	Gs	αs	-	60	-	Nanobody-35	fenoldopam	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z	10.1016/J.CELL.2021.01.028	2021-03-03	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7CKY	7CKY_refined	3.2	R	Active	100	62	Gs	αs	-	60	-	Nanobody-35	CHEMBL3697578	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z	10.1016/J.CELL.2021.01.028	2021-03-03	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7CRH	7CRH_refined	3.3	R	Active	100	61	Gs	αs	-	60	-	Nanobody-35	CHEMBL1416789	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z	10.1016/J.CELL.2021.01.028	2021-03-03	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7LJD	-	3.2	R	Active	100	64	Gs	αs	Engineered G alpha	58	-	Nanobody-35	dopamine LY3154207	small-molecule small-molecule	Agonist PAM	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Singh N, Singh D, Bhide A, Sharma R, Bhowmick S, Patel V, Modi D	10.1101/2021.02.07.430101	2021-03-03	Yes
DRD3	D₃	Dopamine	A	Human	cryo-EM	7CMV	7CMV_refined	2.7	R	Active	100	68	Gi/o	αi1	-	64	BRIL	scFv16	CHEMBL70565	small-molecule	Agonist	dopamine	small-molecule	Yes	No	Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE	10.1016/J.MOLCEL.2021.01.003	2021-03-10	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DTU	7DTU_refined	4.4	A	Intermediate	-	72	-	-	-	-	-	-	L-tryptophan	small-molecule	PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C	10.1038/S41422-021-00474-0	2021-03-10	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DTW	7DTW_refined	4.5	A	Inactive	-	72	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Ling S, Shi P, Liu S, Meng X, Zhou Y, Sun W, Chang S, Zhang X, Zhang L, Shi C, Sun D, Liu L, Tian C	10.1038/S41422-021-00474-0	2021-03-10	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	7ARO	7ARO_refined	3.1	A	Inactive	1	72	-	-	-	-	BRIL	-	CHEMBL124345	small-molecule	Agonist (partial)	adenosine	small-molecule	Yes	Yes	Amelia T, van Veldhoven JPD, Falsini M, Liu R, Heitman LH, van Westen GJP, Segala E, Verdon G, Cheng RKY, Cooke RM, van der Es D, IJzerman AP	10.1021/ACS.JMEDCHEM.0C01856	2021-04-07	Yes
5HT1A	5-HT_1A	5-Hydroxytryptamine	A	Human	cryo-EM	7E2X	7E2X_refined	3.0	R	Active	100	66	Gi/o	αi1	-	62	-	-	Apo (no ligand)	none	Apo (no ligand)	5-hydroxytryptamine	small-molecule	Yes	No	Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE	10.1038/S41586-021-03376-8	2021-04-14	Yes
5HT1A	5-HT_1A	5-Hydroxytryptamine	A	Human	cryo-EM	7E2Z	7E2Z_refined	3.1	R	Active	100	66	Gi/o	αi1	-	62	-	-	aripiprazole	small-molecule	Agonist (partial)	5-hydroxytryptamine	small-molecule	Yes	No	Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE	10.1038/S41586-021-03376-8	2021-04-14	Yes
DRD1	D₁	Dopamine	A	Human	X-ray	7JOZ	7JOZ_refined	3.8	R	Active	100	64	Gs	αs	-	86	-	Nanobody-35	CHEMBL4453318	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2021-04-14	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7AUE	7AUE_refined	3.0	R	Active	100	79	Gs	αs	-	59	-	scFv16	setmelanotide	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M	10.1126/SCIENCE.ABF7958	2021-04-28	Yes
PE2R2	EP₂	Prostanoid	A	Human	cryo-EM	7CX3	7CX3_refined	2.8	R	Active	100	74	Gs	αs	-	58	-	Nanobody-35	taprenepag	small-molecule	Agonist	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y	10.1126/SCIADV.ABF1268	2021-05-05	Yes
GABR2	GABA_B2	GABA_B	C	Human	cryo-EM	7EB2	7EB2_refined	3.5	D	Active	-	72	Gi/o	αi1	-	99	-	scFv16	(-)-baclofen BHFF	small-molecule small-molecule	Agonist PAM	-	-	No	No	Shen C, Mao C, Xu C, Jin N, Zhang H, Shen DD, Shen Q, Wang X, Hou T, Chen Z, Rondard P, Pin JP, Zhang Y, Liu J	10.1038/S41586-021-03507-1	2021-05-05	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7MBY	7MBY_refined	2.4	R	Active	100	66	Gq/11	αq	Gq-Gs-Gi1 chimera	55	-	-	CHEMBL216166	protein	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	-	-	2021-05-26	Yes
V2R	V₂	Vasopressin and oxytocin	A	Human	cryo-EM	7BB7	7BB7_refined	4.4	A	Active	100	72	Gs	αs	-	55	-	Nanobody-35	vasopressin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B	10.1126/SCIADV.ABG5628	2021-06-02	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7DD5	-	3.2	A	Inactive	-	74	-	-	-	-	-	-	Calcium NPS 2143 L-tryptophan	small-molecule small-molecule small-molecule	Agonist NAM PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X	10.1126/SCIADV.ABG1483	2021-06-16	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7E9G	7E9G_refined	3.5	R	Intermediate	-	88	Gi/o	αi1	-	63	-	scFv16	eglumegad JNJ-40411813	small-molecule small-molecule	Agonist PAM	L-glutamic acid	small-molecule	No	No	Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B	10.1038/S41586-021-03495-2	2021-06-23	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7EPA	7EPA_refined	3.6	A	Intermediate	-	90	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
GRM7	mGlu₇	Metabotropic glutamate	C	Human	cryo-EM	7EPC	7EPC_refined	4.0	B	Inactive	-	85	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	L-serine-O-phosphate, L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	X-ray	7EPE	7EPE_refined	2.5	A	Inactive	-	28	-	-	-	-	Flavodoxin	-	CHEMBL3894759	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	Du J, Wang D, Fan H, Xu C, Tai L, Lin S, Han S, Tan Q, Wang X, Xu T, Zhang H, Chu X, Yi C, Liu P, Wang X, Zhou Y, Pin JP, Rondard P, Liu H, Liu J, Sun F, Wu B, Zhao Q	10.1038/S41586-021-03641-W	2021-06-23	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7M3E	-	3.2	B	Inactive	-	75	-	-	-	-	-	-	Calcium NPS 2143 L-tryptophan	small-molecule small-molecule small-molecule	Agonist NAM PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03691-0	2021-06-30	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7M3G	7M3G_refined	2.5	A	Active	-	76	-	-	-	-	-	-	Calcium L-tryptophan evocalcet	small-molecule small-molecule small-molecule	Agonist PAM PAM	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Gao Y, Robertson MJ, Rahman SN, Seven AB, Zhang C, Meyerowitz JG, Panova O, Hannan FM, Thakker RV, Brauner-Osborne H, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03691-0	2021-06-30	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7E14	7E14_refined	2.9	R	Active	100	81	Gs	αs	-	48	-	Nanobody-35	N-Tert-butyl-6,7-dichloroquinoxalin-2-amine LY3502970	small-molecule small-molecule	Ago-PAM Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW	10.1038/S41467-021-24058-Z	2021-07-07	Yes
Q3KSP2	BILF1	Unclassified	A	strain GD1	cryo-EM	7JHJ	7JHJ_refined	3.2	R	Active	100	89	Gi/o	αi1	-	62	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC	10.1016/J.IMMUNI.2021.06.001	2021-07-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	7MT8	7MT8_refined	5.8	R	Active	97	93	-	-	-	-	-	GRK1	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Chen Q, Plasencia M, Li Z, Mukherjee S, Patra D, Chen CL, Klose T, Yao XQ, Kossiakoff AA, Chang L, Andrews PC, Tesmer JJG	10.1038/S41586-021-03721-X	2021-07-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	7MT9	7MT9_refined	7.0	R	Active	97	93	-	-	-	-	-	GRK1	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Chen Q, Plasencia M, Li Z, Mukherjee S, Patra D, Chen CL, Klose T, Yao XQ, Kossiakoff AA, Chang L, Andrews PC, Tesmer JJG	10.1038/S41586-021-03721-X	2021-07-07	Yes
OPSD	Rhodopsin	Opsins	A	Bovine	cryo-EM	7MTB	7MTB_refined	4.0	R	Active	97	93	-	-	-	-	-	Fab light chain Fab heavy chain GRK1	Retinal (all-trans)	small-molecule	Agonist	-	-	No	No	Chen Q, Plasencia M, Li Z, Mukherjee S, Patra D, Chen CL, Klose T, Yao XQ, Kossiakoff AA, Chang L, Andrews PC, Tesmer JJG	10.1038/S41586-021-03721-X	2021-07-07	Yes
GRM2	mGlu₂	Metabotropic glutamate	C	Human	cryo-EM	7MTR	7MTR_refined	3.3	A	Active	-	88	-	-	-	-	-	-	2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine L-glutamic acid	small-molecule small-molecule	Ago-PAM Agonist	L-glutamic acid	small-molecule	No	No	Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G	10.1038/S41586-021-03680-3	2021-07-07	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7DUQ	7DUQ_refined	2.5	R	Active	100	83	Gs	αs	-	61	-	Nanobody-35	N-Tert-butyl-6,7-dichloroquinoxalin-2-amine CHEMBL410972	small-molecule protein	Ago-PAM Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW	10.1038/S41467-021-24058-Z	2021-07-14	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	7F1R	7F1R_refined	3.0	R	Active	100	79	Gi/o	αi1	-	61	-	-	CCL5	peptide	Agonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B	10.1038/S41467-021-24438-5	2021-07-14	Yes
CCR5	CCR5	Chemokine	A	Human	cryo-EM	7F1S	7F1S_refined	2.8	R	Active	100	78	Gi/o	αi1	-	61	-	-	Apo (no ligand)	none	Apo (no ligand)	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B	10.1038/S41467-021-24438-5	2021-07-14	Yes
CCR5	CCR5	Chemokine	A	Human	X-ray	7F1T	-	2.6	A	Inactive	16	86	-	-	-	-	Rubredoxin	-	CCL3	peptide	Agonist	CCL14, CCL5, CCL2, CCL4, CCL3, CCL13, CCL8, CCL7, CCL16, CCL11	peptide	No	No	-	-	2021-07-14	Yes
V2R	V₂	Vasopressin and oxytocin	A	Human	cryo-EM	7DW9	-	2.6	R	Active	100	75	Gs	αs	-	56	-	Nanobody-35 scFv16	vasopressin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y	10.1038/S41422-021-00480-2	2021-07-21	Yes
ADRB3	β₃	Adrenoceptors	A	Dog	cryo-EM	7DH5	7DH5_refined	3.2	R	Active	100	68	Gs	αs	-	59	-	Nanobody-35	mirabegron	small-molecule	Agonist	-	-	Yes	No	Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O	10.1016/J.MOLCEL.2021.06.024	2021-08-04	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7DTY	7DTY_refined	3.0	R	Active	100	79	Gs	αs	-	59	-	Nanobody-35	GIP	small-molecule	Agonist	gastric inhibitory polypeptide	peptide	No	No	Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW	10.7554/ELIFE.68719	2021-08-04	Yes
FZD7	FZD₇	Frizzled	F	Human	cryo-EM	7EVW	-	3.2	R	Active	100	59	Gs	αs	-	58	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F	10.1038/S41422-021-00525-6	2021-08-04	Yes
5HT1F	5-HT_1F	5-Hydroxytryptamine	A	Human	cryo-EM	7EXD	7EXD_refined	3.4	R	Active	100	74	Gi/o	αi1	-	62	BRIL	scFv16	lasmiditan	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE	10.1038/S41422-021-00527-4	2021-08-04	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7KI0	-	2.5	R	Active	100	83	Gs	αs	-	53	-	Nanobody-35	semaglutide	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D	10.1016/J.CELREP.2021.109374	2021-08-04	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7KI1	7KI1_refined	2.5	R	Active	100	83	Gs	αs	-	89	-	Nanobody-35	Taspoglutide	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D	10.1016/J.CELREP.2021.109374	2021-08-04	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7DUR	7DUR_refined	3.3	R	Active	100	80	Gs	αs	-	60	-	Nanobody-35	N-Tert-butyl-6,7-dichloroquinoxalin-2-amine	small-molecule	Ago-PAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW	10.1038/S41467-021-24058-Z	2021-08-11	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7EVM	7EVM_refined	2.5	R	Active	100	61	Gs	αs	-	60	-	Nanobody-35	N-Tert-butyl-6,7-dichloroquinoxalin-2-amine	small-molecule	Ago-PAM	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW	10.1038/S41467-021-24058-Z	2021-08-11	Yes
MTR1A	MT₁	Melatonin	A	Human	cryo-EM	7DB6	7DB6_refined	3.3	D	Active	100	79	Gi/o	αi1	-	62	-	scFv16	ramelteon	small-molecule	Agonist	melatonin	small-molecule	Yes	No	Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O	10.1038/S41594-021-00634-1	2021-08-18	Yes
PTH2R	PTH2	Parathyroid hormone	B1	Human	cryo-EM	7F16	7F16_refined	2.8	R	Active	100	68	Gs	αs	-	58	-	Nanobody-35	TIP39	peptide	Agonist	PTHrP-(1-36), TIP39, PTHrP, PTHrP-(1-34) (human), PTH	peptide	No	No	Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW	10.1073/PNAS.2101279118	2021-08-18	Yes
GHSR	ghrelin	Ghrelin	A	Human	cryo-EM	7F9Y	7F9Y_refined	2.9	R	Active	100	78	Gq/11	αq	Engineered G alpha	59	-	Nanobody-35	ghrelin	peptide	Agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	Yes	No	-	-	2021-08-18	Yes
GHSR	ghrelin	Ghrelin	A	Human	cryo-EM	7F9Z	7F9Z_refined	3.2	R	Active	100	77	Gq/11	αq	Engineered G alpha	59	-	Nanobody-35 scFv16	GHRP-6	peptide	Agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	Yes	No	-	-	2021-08-18	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7EZH	7EZH_refined	3.2	D	Active	100	69	Gi/o	αi1	-	61	-	scFv16	CCK-8	peptide	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	-	-	2021-08-25	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7EZK	7EZK_refined	3.1	D	Active	100	69	Gs	αs	-	58	-	-	CCK-8	peptide	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	-	-	2021-08-25	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7EZM	-	2.9	D	Active	100	71	Gq/11	αq	-	63	-	scFv16	CCK-8	peptide	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	-	-	2021-08-25	Yes
PD2R2	DP₂	Prostanoid	A	Human	X-ray	7M8W	7M8W_refined	2.6	A	Inactive	24	83	-	-	-	-	T4-Lysozyme	-	15(R)-15-methyl-PGD₂	small-molecule	Antagonist	PGJ₂, PGD₂, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	Yes	Liu H, Deepak RNVK, Shiriaeva A, Gati C, Batyuk A, Hu H, Weierstall U, Liu W, Wang L, Cherezov V, Fan H, Zhang C	10.1073/PNAS.2102813118	2021-08-25	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	cryo-EM	7FD8	7FD8_refined	3.8	A	Active	-	63	-	-	-	-	-	-	quisqualate	small-molecule	Agonist	L-glutamic acid	small-molecule	No	No	-	-	2021-09-08	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	cryo-EM	7FD9	7FD9_refined	4.0	A	Inactive	-	63	-	-	-	-	-	-	LY341495	small-molecule	Antagonist	L-glutamic acid	small-molecule	No	No	-	-	2021-09-08	Yes
AA1R	A₁	Adenosine	A	Human	cryo-EM	7LD3	7LD3_refined	3.2	R	Active	100	88	Gi/o	αi2	-	59	-	-	adenosine {2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone	small-molecule small-molecule	Agonist PAM	adenosine	small-molecule	Yes	No	-	-	2021-09-08	Yes
AA1R	A₁	Adenosine	A	Human	cryo-EM	7LD4	7LD4_refined	3.3	R	Active	100	88	Gi/o	αi2	-	59	-	-	adenosine	small-molecule	Agonist	adenosine	small-molecule	Yes	No	-	-	2021-09-08	Yes
GRM5	mGlu₅	Metabotropic glutamate	C	Human	X-ray	7P2L	7P2L_refined	2.5	A	Inactive	-	21	-	-	-	-	T4-Lysozyme	-	alloswitch-1	small-molecule	NAM	L-glutamic acid	small-molecule	No	No	-	-	2021-09-08	Yes
AA2AR	A_2A	Adenosine	A	Human	MicroED	7RM5	7RM5_refined	2.8	A	Inactive	1	72	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	Martynowycz MW, Shiriaeva A, Ge X, Hattne J, Nannenga BL, Cherezov V, Gonen T	10.1073/PNAS.2106041118	2021-09-08	Yes
GRM1	mGlu₁	Metabotropic glutamate	C	Human	cryo-EM	7DGD	7DGD_refined	4.0	A	Inactive	-	66	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	L-glutamic acid	small-molecule	No	No	Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T	10.1007/S13238-020-00808-5	2021-09-22	Yes
GRM1	mGlu₁	Metabotropic glutamate	C	Human	cryo-EM	7DGE	7DGE_refined	3.7	A	Intermediate	-	66	-	-	-	-	-	Nanobody-43	quisqualate	small-molecule	Agonist	L-glutamic acid	small-molecule	No	No	Zhang J, Qu L, Wu L, Tang X, Luo F, Xu W, Xu Y, Liu ZJ, Hua T	10.1007/S13238-020-00808-5	2021-09-22	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7E6U	7E6U_refined	6.0	A	Inactive	-	72	-	-	-	-	-	Nanobody-2D11	Apo (no ligand)	none	Apo (no ligand)	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Chen X, Wang L, Cui Q, Ding Z, Han L, Kou Y, Zhang W, Wang H, Jia X, Dai M, Shi Z, Li Y, Li X, Geng Y	10.7554/ELIFE.68578	2021-09-22	Yes
S1PR3	S1P₃	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW2	7EW2_refined	3.1	R	Active	100	77	Gi/o	αi1	-	64	-	scFv16	(S)-FTY720-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z	10.1038/S41422-021-00567-W	2021-09-29	Yes
S1PR3	S1P₃	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW4	-	3.2	R	Active	100	76	Gi/o	αi1	-	64	-	scFv16	CYM-5541	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z	10.1038/S41422-021-00567-W	2021-09-29	Yes
LSHR	LH	Glycoprotein hormone	A	Human	cryo-EM	7FIH	-	3.2	R	Active	100	79	Gs	αs	-	56	-	-	Choriogonadotropin beta Glycoprotein alpha 5-Amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]thieno[2,3-d]pyrimidine-6-carboxamide	protein protein small-molecule	Agonist	LH, hCG	peptide	Yes	No	Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE	10.1038/S41586-021-03924-2	2021-09-29	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	X-ray	7F8U	7F8U_refined	2.8	A	Inactive	1	65	-	-	-	-	T4-Lysozyme	-	lintitript	small-molecule	Antagonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	No	No	Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q	10.1038/S41589-021-00866-8	2021-10-13	Yes
LSHR	LH	Glycoprotein hormone	A	Human	cryo-EM	7FIJ	7FIJ_refined	3.8	R	Inactive	5	80	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	LH, hCG	peptide	Yes	No	Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE	10.1038/S41586-021-03924-2	2021-09-29	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	X-ray	6ZG9	6ZG9_refined	2.5	A	Inactive	3	62	-	-	-	-	T4-Lysozyme	-	7-fluoro-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1H-benzimidazol-2-one	small-molecule	Agonist	acetylcholine	small-molecule	No	No	-	-	2021-10-06	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	X-ray	6ZG4	6ZG4_refined	2.3	A	Inactive	3	62	-	-	-	-	T4-Lysozyme	-	Ethyl (4S)-4-[4-[(1-methylcyclobutyl)carbamoyl]piperidin-1-yl]azepane-1-carboxylate	small-molecule	Agonist	acetylcholine	small-molecule	No	No	-	-	2021-10-06	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	7V3Z	7V3Z_refined	3.3	A	Active	96	60	-	-	-	-	Flavodoxin	-	CP55940	small-molecule	Agonist	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Wang X, Liu D, Shen L, Li F, Li Y, Yang L, Xu T, Tao H, Yao D, Wu L, Hirata K, Bohn LM, Makriyannis A, Liu X, Hua T, Liu ZJ, Wang J	10.1021/JACS.1C06847	2021-11-24	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	X-ray	7F8Y	7F8Y_refined	2.5	A	Inactive	1	65	-	-	-	-	T4-Lysozyme	-	DEVAZEPIDE	small-molecule	Antagonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	No	No	-	-	2021-10-13	Yes
ACM1	M₁	Acetylcholine (muscarinic)	A	Human	X-ray	6ZFZ	6ZFZ_refined	2.2	A	Inactive	3	62	-	-	-	-	T4-Lysozyme	-	CHEMBL3354065	small-molecule	Agonist	acetylcholine	small-molecule	No	No	-	-	2021-10-06	Yes
GASR	CCK₂	Cholecystokinin	A	Human	cryo-EM	7F8W	7F8W_refined	3.1	R	Active	100	62	Gq/11	αq	Gq-Gi1 chimera	62	-	scFv16	desulfated gastrin-17	peptide	Agonist	CCK-4, gastrin-17, gastrin-71, desulfated cholecystokinin-8, desulfated gastrin-34, desulfated gastrin-71, gastrin-14, desulfated gastrin-14, CCK-33, gastrin-34, CCK-58, CCK-39, CCK-8, desulfated gastrin-17	peptide	Yes	No	-	-	2021-10-13	Yes
GASR	CCK₂	Cholecystokinin	A	Human	cryo-EM	7F8V	7F8V_refined	3.3	R	Active	100	62	Gi/o	αi2	-	61	-	-	desulfated gastrin-17	peptide	Agonist	CCK-4, gastrin-17, gastrin-71, desulfated cholecystokinin-8, desulfated gastrin-34, desulfated gastrin-71, gastrin-14, desulfated gastrin-14, CCK-33, gastrin-34, CCK-58, CCK-39, CCK-8, desulfated gastrin-17	peptide	Yes	No	-	-	2021-10-13	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7F55	7F55_refined	3.1	R	Active	100	82	Gs	αs	-	58	-	Nanobody-35	bremelanotide	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	-	10.1038/S41422-021-00552-3	2021-11-03	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7PIV	7PIV_refined	2.9	R	Active	100	78	Gs	αs	-	46	-	Nanobody-35	afamelanotide	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	-	-	2021-11-17	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7RTB	7RTB_refined	2.1	R	Active	100	83	Gs	αs	-	60	-	Nanobody-35	Peptide-19	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	-	10.1016/J.BBRC.2021.09.016	2021-10-06	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7S8O	7S8O_refined	2.6	R	Active	100	78	Gi/o	αi1	-	62	BRIL	scFv16	(R)-ZINC-3573	small-molecule	Agonist	PAMP-20	peptide	No	No	-	-	2021-11-17	Yes
BKRB1	B₁	Bradykinin	A	Human	cryo-EM	7EIB	7EIB_refined	3.0	A	Active	100	84	Gq/11	αq	Gq-Gi1 chimera	61	-	-	[des-Arg¹⁰]kallidin	peptide	Agonist	[Hyp³]bradykinin, [des-Arg¹⁰]kallidin, Lys-[Hyp³]-bradykinin, kallidin, T-kinin, [des-Arg⁹]bradykinin, bradykinin	peptide	Yes	No	-	10.1038/S41594-021-00645-Y	2021-10-13	Yes
GP158	GPR158	C Orphans	C	Human	cryo-EM	7SHE	7SHE_refined	3.4	A	Inactive	-	45	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Patil DN, Singh S, Laboute T, Strutzenberg TS, Qiu X, Wu D, Novick SJ, Robinson CV, Griffin PR, Hunt JF, Izard T, Singh AK, Martemyanov KA	34793198	2021-12-01	Yes
NK1R	NK₁	Tachykinin	A	Human	cryo-EM	7RMH	7RMH_refined	3.1	R	Active	100	70	Gs	αs	-	55	-	Nanobody-35	substance P	peptide	Agonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	-	10.1038/S41589-021-00890-8	2021-11-03	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7F58	7F58_refined	3.1	R	Active	100	82	Gs	αs	-	58	-	Nanobody-35	THIQ	small-molecule	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	-	-	2021-11-03	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7S8L	7S8L_refined	2.5	R	Active	100	76	Gq/11	αq	Gq-Gs chimera	57	-	scFv16	Cortistatin 14	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-11-17	Yes
NK1R	NK₁	Tachykinin	A	Human	cryo-EM	7RMG	7RMG_refined	3.0	R	Active	100	71	Gs	αs	Gs-Gq chimera	49	-	Nanobody-35	substance P	peptide	Agonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	-	-	2021-11-03	Yes
LSHR	LH	Glycoprotein hormone	A	Human	cryo-EM	7FII	-	4.3	R	Active	100	82	Gs	αs	-	91	-	-	Choriogonadotropin beta Glycoprotein alpha	protein protein	Agonist	LH, hCG	peptide	Yes	No	Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE	10.1038/S41586-021-03924-2	2021-09-29	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7F54	7F54_refined	3.0	R	Active	100	82	Gs	αs	-	58	-	Nanobody-35	afamelanotide	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	-	-	2021-11-03	Yes
NK1R	NK₁	Tachykinin	A	Human	cryo-EM	7RMI	7RMI_refined	3.2	R	Active	100	70	Gs	αs	Gs-Gq chimera	49	-	Nanobody-35	substance P	peptide	Agonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	-	-	2021-11-03	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7S8N	7S8N_refined	2.9	R	Active	100	76	Gq/11	αq	Gq-Gs chimera	57	-	scFv16	(R)-ZINC-3573	small-molecule	Agonist	PAMP-20	peptide	No	No	-	-	2021-11-17	Yes
MRGX4	MRGPRX4	A orphans	A	Human	cryo-EM	7S8P	7S8P_refined	2.6	R	Active	100	77	Gq/11	αq	Gq-Gs chimera	57	BRIL	scFv16	N-[(1r,3R,5S,7R)-3,5-dimethyltricyclo[3.3.1.1~3,7~]decane-1-carbonyl]-D-phenylalanine	small-molecule	Agonist	-	-	No	No	-	-	2021-11-17	Yes
BKRB2	B₂	Bradykinin	A	Human	cryo-EM	7F2O	7F2O_refined	2.9	R	Active	100	73	Gq/11	αq	Gq-Gi1 chimera	60	-	scFv16	bradykinin	peptide	Agonist	[Hyp³]bradykinin, [des-Arg¹⁰]kallidin, Lys-[Hyp³]-bradykinin, kallidin, T-kinin, [des-Arg⁹]bradykinin, bradykinin	peptide	Yes	No	-	-	2021-10-13	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7PIU	-	2.6	R	Active	100	78	Gs	αs	-	48	-	Nanobody-35	setmelanotide	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P	10.1038/S41422-021-00569-8	2021-11-17	Yes
MC4R	MC₄	Melanocortin	A	Human	cryo-EM	7F53	7F53_refined	3.0	R	Active	100	82	Gs	αs	-	58	-	Nanobody-35	α-MSH	peptide	Agonist	ACTH, β-MSH, α-MSH, γ-MSH, agouti-related protein	peptide	Yes	No	-	-	2021-11-03	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7S8M	7S8M_refined	2.5	R	Active	100	77	Gi/o	αi1	-	62	BRIL	scFv16	Cortistatin 14	peptide	Agonist	PAMP-20	peptide	No	No	Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL	10.1038/S41586-021-04126-6	2021-11-17	Yes
GP158	GPR158	C Orphans	C	Human	cryo-EM	7EWL	7EWL_refined	3.5	A	Inactive	-	41	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	-	10.1038/S41467-021-27147-1	2021-12-01	Yes
GP158	GPR158	C Orphans	C	Human	cryo-EM	7SHF	7SHF_refined	3.4	B	Inactive	-	23	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Patil DN, Singh S, Laboute T, Strutzenberg TS, Qiu X, Wu D, Novick SJ, Robinson CV, Griffin PR, Hunt JF, Izard T, Singh AK, Martemyanov KA	34793198	2021-12-01	Yes
GP158	GPR158	C Orphans	C	Human	cryo-EM	7EWP	7EWP_refined	4.3	A	Inactive	-	47	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	-	-	2021-12-01	Yes
GP158	GPR158	C Orphans	C	Human	cryo-EM	7EWR	7EWR_refined	4.7	A	Inactive	-	47	-	-	-	-	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VDH	7VDH_refined	2.9	R	Active	100	81	Gi/o	αi1	-	62	-	scFv16	compound 48/80	small-molecule	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VDL	7VDL_refined	3.2	R	Active	100	78	Gi/o	αi1	-	61	-	scFv16	Cortistatin 14	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VDM	7VDM_refined	3.0	R	Active	100	77	Gi/o	αi1	-	61	-	scFv16	substance P	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VUY	-	2.8	R	Active	100	78	Gi/o	αi1	-	64	-	scFv16	PAMP-12	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VUZ	-	2.9	R	Active	100	76	Gi/o	αi1	-	62	-	scFv16	PAMP-12	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VV0	7VV0_refined	3.5	R	Active	97	80	-	-	-	-	-	-	PAMP-12	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VV3	-	3.0	R	Active	100	79	Gi/o	αi1	-	62	-	scFv16	Cortistatin 14	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VV4	7VV4_refined	3.0	R	Active	97	80	-	-	-	-	-	-	Cortistatin 14	peptide	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VV5	7VV5_refined	2.8	R	Active	100	81	Gi/o	αi1	-	64	-	scFv16	compound 48/80	small-molecule	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
MRGX2	MRGPRX2	A orphans	A	Human	cryo-EM	7VV6	7VV6_refined	3.3	R	Active	97	82	-	-	-	-	-	-	compound 48/80	small-molecule	Agonist	PAMP-20	peptide	No	No	-	-	2021-12-01	Yes
GHSR	ghrelin	Ghrelin	A	Human	cryo-EM	7NA7	7NA7_refined	2.7	R	Active	100	80	Gi/o	αi1	-	61	-	Antibody fragment	Ghrelin-27	peptide	Agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	No	No	Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C	10.1038/S41467-021-26735-5	2021-12-15	Yes
GHSR	ghrelin	Ghrelin	A	Human	cryo-EM	7NA8	7NA8_refined	2.7	R	Active	100	78	Gi/o	αi1	-	61	-	Antibody fragment	ibutamoren	small-molecule	Agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	No	No	Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C	10.1038/S41467-021-26735-5	2021-12-15	Yes
NK1R	NK₁	Tachykinin	A	Human	cryo-EM	7P00	7P00_refined	2.7	R	Active	100	71	Gq/11	αq	Gq-Gs-Gi1 chimera	59	-	scFv16	substance P	peptide	Agonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A	10.1126/SCIADV.ABK2872	2021-12-15	Yes
NK1R	NK₁	Tachykinin	A	Human	cryo-EM	7P02	7P02_refined	2.9	R	Active	100	71	Gs	αs	Gs-Gi1 chimera	57	-	scFv16	substance P	peptide	Agonist	neurokinin A, neuropeptide-γ, neuropeptide K, substance P, neurokinin B, hemokinin 1	peptide	Yes	No	Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A	10.1126/SCIADV.ABK2872	2021-12-15	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7VOD	7VOD_refined	3.3	A	Inactive	1	58	-	-	-	-	BRIL	-	cariprazine	small-molecule	Agonist (partial)	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Chen Z, Fan L, Wang H, Yu J, Lu D, Qi J, Nie F, Luo Z, Liu Z, Cheng J, Wang S	10.1038/S41593-021-00971-W	2021-12-22	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7VOE	7VOE_refined	2.9	A	Inactive	1	58	-	-	-	-	BRIL	-	aripiprazole	small-molecule	Agonist (partial)	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Chen Z, Fan L, Wang H, Yu J, Lu D, Qi J, Nie F, Luo Z, Liu Z, Cheng J, Wang S	10.1038/S41593-021-00971-W	2021-12-22	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	X-ray	7F8X	7F8X_refined	3.0	A	Inactive	1	66	-	-	-	-	T4-Lysozyme	-	NN9056	peptide	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q	10.1038/S41589-021-00866-8	2021-12-29	Yes
GP139	GPR139	A orphans	A	Human	cryo-EM	7VUG	7VUG_refined	3.2	R	Active	100	80	Gi/o	αi1	-	62	-	scFv16	JNJ-63533054	small-molecule	Agonist	L-tryptophan, L-phenylalanine	small-molecule	Yes	No	Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ	10.1038/S41422-021-00591-W	2021-12-29	Yes
GP139	GPR139	A orphans	A	Human	cryo-EM	7VUI	-	3.3	R	Active	100	79	Gs	αs	-	57	-	Nanobody-35	JNJ-63533054	small-molecule	Agonist	L-tryptophan, L-phenylalanine	small-molecule	Yes	No	Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ	10.1038/S41422-021-00591-W	2021-12-29	Yes
GP139	GPR139	A orphans	A	Human	cryo-EM	7VUH	-	3.2	R	Active	100	80	Gs	αs	-	59	-	Nanobody-35	JNJ-63533054	small-molecule	Agonist	L-tryptophan, L-phenylalanine	small-molecule	Yes	No	Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ	10.1038/S41422-021-00591-W	2021-12-29	Yes
GP139	GPR139	A orphans	A	Human	cryo-EM	7VUJ	-	3.8	R	Active	100	79	Gs	αs	-	58	-	Nanobody-35	JNJ-63533054	small-molecule	Agonist	L-tryptophan, L-phenylalanine	small-molecule	Yes	No	Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ	10.1038/S41422-021-00591-W	2021-12-29	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7S1M	7S1M_refined	2.4	R	Active	100	82	Gs	αs	-	59	-	Nanobody-35	exendin-4	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH	10.1038/S41589-021-00945-W	2022-01-05	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7S3I	-	2.5	R	Active	100	57	Gs	αs	-	59	-	Nanobody-35	exendin-4	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH	10.1038/S41589-021-00945-W	2022-01-05	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EO2	7EO2_refined	2.9	A	Active	100	73	Gi/o	αi1	-	62	-	scFv16	(S)-FTY720-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y	10.1038/S41589-021-00930-3	2022-01-05	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EO4	7EO4_refined	2.9	A	Active	100	74	Gi/o	αi1	-	43	-	scFv16	siponimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y	10.1038/S41589-021-00930-3	2022-01-05	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7WF7	7WF7_refined	3.4	A	Active	100	71	Gi/o	αi1	-	40	-	scFv16	sphingosine 1-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y	10.1038/S41589-021-00930-3	2022-01-05	Yes
ADA1B	α_1B	Adrenoceptors	A	Human	X-ray	7B6W	-	2.9	A	Inactive	1	51	-	-	-	-	DARPin D12	-	(+)-cyclazosin	small-molecule	Inverse agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Deluigi M, Morstein L, Schuster M, Klenk C, Merklinger L, Cridge RR, de Zhang LA, Klipp A, Vacca S, Vaid TM, Mittl PRE, Egloff P, Eberle SA, Zerbe O, Chalmers DK, Scott DJ, Pluckthun A	10.1038/s41467-021-27911-3	2022-01-12	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC4	7WC4_refined	3.2	A	Inactive	1	61	-	-	-	-	BRIL	-	5-hydroxytryptamine	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC6	7WC6_refined	2.6	A	Inactive	1	58	-	-	-	-	BRIL	-	Lysergide	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC5	7WC5_refined	3.2	A	Inactive	1	60	-	-	-	-	BRIL	-	psilocin	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC7	7WC7_refined	2.6	A	Inactive	1	59	-	-	-	-	BRIL	-	lisuride	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC8	7WC8_refined	2.5	A	Inactive	1	59	-	-	-	-	BRIL	-	LUMATEPERONE	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	X-ray	7WC9	7WC9_refined	2.5	A	Inactive	1	59	-	-	-	-	BRIL	-	(10~{R},15~{S})-12-[3-(2-methoxyphenyl)propyl]-4-methyl-1,4,12-triazatetracyclo[7.6.1.0^{5,16}.0^{10,15}]hexadeca-5(16),6,8-triene	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	No	No	Cao D, Yu J, Wang H, Luo Z, Liu X, He L, Qi J, Fan L, Tang L, Chen Z, Li J, Cheng J, Wang S	10.1126/SCIENCE.ABL8615	2022-01-26	Yes
GHSR	ghrelin	Ghrelin	A	Human	X-ray	7F83	7F83_refined	2.9	A	Inactive	13	78	-	-	-	-	BRIL	-	PF-05190457	small-molecule	Inverse agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	No	No	Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z	10.1038/S41467-022-27975-9	2022-01-19	Yes
GHSR	ghrelin	Ghrelin	A	Human	cryo-EM	7W2Z	7W2Z_refined	2.8	R	Active	100	82	Gi/o	αo	-	60	-	scFv16	Ghrelin	peptide	Agonist	ghrelin, [des-Gln¹⁴]ghrelin	peptide	Yes	No	Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z	10.1038/S41467-022-27975-9	2022-01-19	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7LLL	7LLL_refined	3.7	R	Active	100	79	Gs	αs	-	59	-	Nanobody-35	exendin-4	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D	10.1038/S41467-021-27760-0	2022-01-12	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7LLY	7LLY_refined	3.3	R	Active	100	77	Gs	αs	-	50	-	Nanobody-35	Pro-glucagon	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D	10.1038/S41467-021-27760-0	2022-01-12	Yes
US28	US28	Unclassified	A	strain AD169	cryo-EM	7RKF	-	4.0	R	Active	100	84	Gq/11	α11	-	96	-	scFv16	Fractalkine	peptide	Agonist	-	-	Yes	No	Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC	10.1126/SCIADV.ABL5442	2022-01-26	Yes
US28	US28	Unclassified	A	strain AD169	cryo-EM	7RKM	7RKM_refined	3.5	R	Active	100	83	Gi/o	αi1	-	61	-	scFv16	Fractalkine	peptide	Agonist	-	-	Yes	No	Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC	10.1126/SCIADV.ABL5442	2022-01-26	Yes
US28	US28	Unclassified	A	strain AD169	cryo-EM	7RKN	7RKN_refined	3.6	R	Active	100	83	Gi/o	αi1	-	61	-	scFv16	Fractalkine	peptide	Agonist	-	-	Yes	No	Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC	10.1126/SCIADV.ABL5442	2022-01-26	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7SIL	7SIL_refined	2.7	A	Active	-	72	-	-	-	-	-	-	tecalcet Cyclomethyltryptophan	small-molecule small-molecule	Agonist	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR	10.1073/PNAS.2115849118	2022-01-19	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7SIN	7SIN_refined	5.9	A	Inactive	-	74	-	-	-	-	-	-	NPS 2143	small-molecule	Antagonist	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR	10.1073/PNAS.2115849118	2022-01-19	Yes
CASR	CaS	Calcium-sensing	C	Human	cryo-EM	7SIM	7SIM_refined	2.7	A	Active	-	72	-	-	-	-	-	-	Cyclomethyltryptophan	small-molecule	Agonist	L-tryptophan, Ca²⁺, spermine, Mg²⁺	small-molecule	No	No	Park J, Zuo H, Frangaj A, Fu Z, Yen LY, Zhang Z, Mosyak L, Slavkovich VN, Liu J, Ray KM, Cao B, Vallese F, Geng Y, Chen S, Grassucci R, Dandey VP, Tan YZ, Eng E, Lee Y, Kloss B, Liu Z, Hendrickson WA, Potter CS, Carragher B, Graziano J, Conigrave AD, Frank J, Clarke OB, Fan QR	10.1073/PNAS.2115849118	2022-01-19	Yes
GHRHR	GHRH	Glucagon	B1	Human	cryo-EM	7V9M	7V9M_refined	3.3	R	Active	100	63	Gs	αs	-	57	-	Nanobody-35	Somatoliberin	peptide	Agonist	GHRH	peptide	No	No	-	-	2021-10-20	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EVY	7EVY_refined	3.0	D	Active	100	71	Gi/o	αi1	-	64	-	scFv16	siponimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z	10.1038/S41422-021-00566-X	2021-09-29	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EVZ	7EVZ_refined	3.1	D	Active	100	71	Gi/o	αi1	-	64	-	scFv16	cenerimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z	10.1038/S41422-021-00566-X	2021-09-29	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW0	7EW0_refined	3.4	D	Active	100	71	Gi/o	αi1	-	64	-	scFv16	ozanimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z	10.1038/S41422-021-00566-X	2021-09-29	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7EW7	7EW7_refined	3.3	D	Active	100	75	Gi/o	αi1	-	64	-	scFv16	SEW2871	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z	10.1038/S41422-021-00566-X	2021-09-29	Yes
MSHR	MC₁	Melanocortin	A	Human	cryo-EM	7F4D	7F4D_refined	3.0	R	Active	100	83	Gs	αs	-	59	-	Nanobody-35	INTERMEDINE	protein	Agonist	β-MSH, α-MSH, γ-MSH, ACTH	peptide	Yes	No	Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE	10.1038/S41422-021-00557-Y	2021-09-08	Yes
MSHR	MC₁	Melanocortin	A	Human	cryo-EM	7F4F	7F4F_refined	2.9	R	Active	100	85	Gs	αs	-	59	-	scFv16	CHEMBL407070	protein	Agonist	β-MSH, α-MSH, γ-MSH, ACTH	peptide	Yes	No	Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE	10.1038/S41422-021-00557-Y	2021-09-08	Yes
MSHR	MC₁	Melanocortin	A	Human	cryo-EM	7F4H	7F4H_refined	2.7	R	Active	100	84	Gs	αs	-	59	-	Nanobody-35 scFv16	CHEMBL407070	protein	Agonist	β-MSH, α-MSH, γ-MSH, ACTH	peptide	Yes	No	Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE	10.1038/S41422-021-00557-Y	2021-09-08	Yes
MSHR	MC₁	Melanocortin	A	Human	cryo-EM	7F4I	7F4I_refined	3.1	R	Active	100	84	Gs	αs	-	59	-	Nanobody-35	bremelanotide	peptide	Agonist	β-MSH, α-MSH, γ-MSH, ACTH	peptide	Yes	No	Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE	10.1038/S41422-021-00557-Y	2021-09-08	Yes
AGTR2	AT₂	Angiotensin	A	Human	X-ray	7JNI	7JNI_refined	3.0	A	Active	99	82	-	-	-	-	BRIL	-	olodanrigan	small-molecule	Antagonist	angiotensin-(1-7), angiotensin II, angiotensin III	peptide	Yes	No	-	-	2022-02-09	Yes
FPR1	FPR1	Formylpeptide	A	Human	cryo-EM	7T6T	7T6T_refined	3.2	R	Active	100	85	Gi/o	αi1	-	61	-	-	synthetic peptide	peptide	Agonist	fMet-Leu-Phe, annexin I, spinorphin, cathepsin G	peptide	Yes	No	-	-	2022-03-30	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7T6S	7T6S_refined	3.0	R	Active	100	85	Gi/o	αi1	-	61	-	scFv16	N-(4-chlorophenyl)-N'-[1-methyl-3-oxo-2-phenyl-5-(propan-2-yl)-2,3-dihydro-1H-pyrazol-4-yl]urea	small-molecule	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	-	-	2022-03-30	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7T6U	7T6U_refined	2.9	R	Active	100	85	Gi/o	αi1	-	62	-	-	synthetic peptide	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	-	-	2022-03-30	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7T6V	7T6V_refined	3.1	R	Active	100	85	Gi/o	αi1	-	61	-	scFv16	synthetic peptide	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	-	-	2022-03-30	Yes
NPY1R	Y₁	Neuropeptide Y	A	Human	cryo-EM	7VGX	7VGX_refined	3.2	R	Active	100	73	Gi/o	αi1	-	63	-	scFv16	neuropeptide Y	peptide	Agonist	pancreatic polypeptide, neuropeptide Y, peptide YY	peptide	Yes	No	Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ	10.1038/S41467-022-28510-6	2022-02-23	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7T10	7T10_refined	2.5	R	Active	100	78	Gi/o	αi3	-	62	-	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G	10.1038/S41594-022-00727-5	2022-03-09	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7T11	7T11_refined	2.7	R	Active	100	77	Gi/o	αi3	-	62	-	scFv16	Octreotide	peptide	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G	10.1038/S41594-022-00727-5	2022-03-09	Yes
OXYR	OT	Vasopressin and oxytocin	A	Human	cryo-EM	7RYC	-	2.9	O	Active	100	73	Gq/11	αq	Gamma subunit fused to alpha subunit	57	-	scFv16	oxytocin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G	10.1038/S41594-022-00728-4	2022-03-09	Yes
CCR1	CCR1	Chemokine	A	Human	cryo-EM	7VL8	7VL8_refined	2.9	R	Active	100	80	Gi/o	αi1	-	62	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	CCL14, CCL5, CCL4, CCL23, CCL3, CCL13, CCL8, CCL7, CCL15, CCL16	peptide	No	No	Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H	10.1038/S41589-021-00918-Z	2022-03-23	Yes
CCR1	CCR1	Chemokine	A	Human	cryo-EM	7VL9	7VL9_refined	2.6	R	Active	100	85	Gi/o	αi1	-	62	-	scFv16	CCL15(26-92)	peptide	Agonist	CCL14, CCL5, CCL4, CCL23, CCL3, CCL13, CCL8, CCL7, CCL15, CCL16	peptide	No	No	Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H	10.1038/S41589-021-00918-Z	2022-03-23	Yes
CCR1	CCR1	Chemokine	A	Human	cryo-EM	7VLA	7VLA_refined	2.7	R	Active	100	85	Gi/o	αi1	-	64	-	scFv16	CCL15(27-92)	peptide	Agonist	CCL14, CCL5, CCL4, CCL23, CCL3, CCL13, CCL8, CCL7, CCL15, CCL16	peptide	No	No	Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H	10.1038/S41589-021-00918-Z	2022-03-23	Yes
LT4R1	BLT₁	Leukotriene	A	Human	cryo-EM	7VKT	7VKT_refined	2.9	A	Active	100	82	Gi/o	αi1	-	64	-	scFv16	LTB₄	small-molecule	Agonist	LTB₄, 20-hydroxy-LTB₄, 12R-HETE	small-molecule	Yes	No	Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y	10.1038/S41467-022-28820-9	2022-03-09	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7TD0	7TD0_refined	2.8	R	Active	100	80	Gi/o	αi1	-	62	-	-	(2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY	10.1038/S41467-022-28417-2	2022-02-09	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7TD1	7TD1_refined	3.1	R	Active	100	80	Gi/o	αi1	-	62	-	-	(2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY	10.1038/S41467-022-28417-2	2022-02-09	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7TD2	7TD2_refined	3.1	R	Active	100	80	Gi/o	αi1	-	62	-	-	(2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY	10.1038/S41467-022-28417-2	2022-02-09	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7TD3	7TD3_refined	3.0	R	Active	100	76	Gi/o	αi1	-	63	-	-	sphingosine 1-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY	10.1038/S41467-022-28417-2	2022-02-09	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7TD4	7TD4_refined	2.6	R	Active	100	76	Gi/o	αi1	-	63	-	-	siponimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY	10.1038/S41467-022-28417-2	2022-02-09	Yes
MTR1A	MT₁	Melatonin	A	Human	cryo-EM	7VGZ	7VGZ_refined	3.3	B	Active	100	81	Gi/o	αi1	-	62	-	scFv16	ramelteon	small-molecule	Agonist	melatonin	small-molecule	Yes	No	-	-	2022-03-02	Yes
MTR1A	MT₁	Melatonin	A	Human	cryo-EM	7VGY	7VGY_refined	3.1	A	Active	100	80	Gi/o	αi1	-	62	-	scFv16	2-iodo-melatonin	small-molecule	Agonist	melatonin	small-molecule	Yes	No	-	-	2022-03-02	Yes
MTR1B	MT₂	Melatonin	A	Human	cryo-EM	7VH0	7VH0_refined	3.5	A	Active	100	75	Gi/o	αi1	-	61	-	scFv16	ramelteon	small-molecule	Agonist	melatonin	small-molecule	Yes	No	-	-	2022-03-02	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	7PX4	7PX4_refined	2.3	A	Inactive	1	72	-	-	-	-	BRIL	-	Preladenant conjugate PSB-2113	small-molecule	Antagonist	adenosine	small-molecule	No	No	Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE	10.1002/ANIE.202115545	2022-03-02	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	7PYR	7PYR_refined	2.6	A	Inactive	1	72	-	-	-	-	BRIL	-	Preladenant conjugate PSB-2115	small-molecule	Antagonist	adenosine	small-molecule	No	No	Claff T, Klapschinski TA, Tiruttani Subhramanyam UK, Vaassen VJ, Schlegel JG, Vielmuth C, Voss JH, Labahn J, Muller CE	10.1002/ANIE.202115545	2022-03-02	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYF	-	2.2	R	Active	100	77	Gs	αs	-	58	-	Nanobody-35 RAMP1	amylin peptide	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYH	7TYH_refined	3.3	R	Active	100	78	Gs	αs	-	58	-	Nanobody-35	Calcitonin human	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYI	7TYI_refined	3.3	R	Active	100	77	Gs	αs	-	58	-	Nanobody-35	Amylin rat	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-30	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYL	7TYL_refined	3.3	R	Active	100	78	Gs	αs	-	58	-	Nanobody-35	Amylin rat	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYN	7TYN_refined	2.6	R	Active	100	79	Gs	αs	-	58	-	Nanobody-35	Calcitonin salmon	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-30	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYO	7TYO_refined	2.7	R	Active	100	76	Gs	αs	-	58	-	Nanobody-35	Calcitonin human	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYW	7TYW_refined	3.0	R	Active	100	78	Gs	αs	-	58	-	Nanobody-35	Calcitonin salmon	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYX	-	2.6	R	Active	100	77	Gs	αs	-	59	-	Nanobody-35	Amylin rat	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-30	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TYY	7TYY_refined	3.0	R	Active	100	78	Gs	αs	-	58	-	Nanobody-35	Calcitonin salmon	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
CALCR	CT	Calcitonin	B1	Human	cryo-EM	7TZF	-	2.4	R	Active	100	77	Gs	αs	-	59	-	Nanobody-35 RAMP3	amylin peptide	peptide	Agonist	amylin, calcitonin, adrenomedullin, calcitonin (salmon), adrenomedullin 2/intermedin, α-CGRP, β-CGRP	peptide	No	No	-	-	2022-03-23	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7FIN	7FIN_refined	3.1	R	Active	100	82	Gs	αs	-	59	-	Nanobody-35	Peptide-20	peptide	Agonist	gastric inhibitory polypeptide	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-02-23	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7FIY	7FIY_refined	3.4	R	Active	100	77	Gs	αs	-	60	-	Nanobody-35	tirzepatide	peptide	Agonist	gastric inhibitory polypeptide	peptide	No	No	-	-	2022-03-02	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7VAB	7VAB_refined	3.2	R	Active	100	58	Gs	αs	Mini-Gs	60	-	Nanobody-35	tirzepatide	peptide	Agonist	gastric inhibitory polypeptide	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-03-02	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7FIM	7FIM_refined	3.4	R	Active	100	83	Gs	αs	-	57	-	Nanobody-35	tirzepatide	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-03-02	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7VBI	7VBI_refined	3.0	R	Active	100	83	Gs	αs	Mini-Gs	58	-	-	tirzepatide	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-03-02	Yes
GLR	glucagon	Glucagon	B1	Human	cryo-EM	7V35	7V35_refined	3.4	R	Active	100	82	Gs	αs	-	53	-	Nanobody-35	Peptide-20	peptide	Agonist	glucagon	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-03-02	Yes
GRM3	mGlu₃	Metabotropic glutamate	C	Human	cryo-EM	7WI6	7WI6_refined	3.7	A	Inactive	-	82	-	-	-	-	-	-	LY341495	small-molecule	Antagonist	NAAG, L-glutamic acid	small-molecule	No	No	Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J	10.1038/S41422-022-00623-Z	2022-03-16	Yes
GRM3	mGlu₃	Metabotropic glutamate	C	Human	cryo-EM	7WI8	7WI8_refined	4.2	A	Inactive	-	82	-	-	-	-	-	-	LY341495	small-molecule	Antagonist	NAAG, L-glutamic acid	small-molecule	No	No	Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J	10.1038/S41422-022-00623-Z	2022-03-16	Yes
GRM3	mGlu₃	Metabotropic glutamate	C	Human	cryo-EM	7WIH	7WIH_refined	3.7	A	Active	-	84	-	-	-	-	-	-	CHEMBL4081453	small-molecule	Agonist	NAAG, L-glutamic acid	small-molecule	No	No	Fang W, Yang F, Xu C, Ling S, Lin L, Zhou Y, Sun W, Wang X, Liu P, Rondard P, Shi P, Pin JP, Tian C, Liu J	10.1038/S41422-022-00623-Z	2022-03-16	Yes
GPR88	GPR88	A orphans	A	Human	cryo-EM	7EJX	7EJX_refined	2.4	R	Active	100	60	Gi/o	αi1	-	61	-	scFv16	compound 2 [PMID: 24793972]	small-molecule	PAM	-	-	Yes	No	-	-	2022-04-13	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7WIC	7WIC_refined	2.8	R	Active	100	78	Gi/o	αi1	-	64	-	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C	10.1038/S41422-022-00669-Z	2022-06-01	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7X8R	-	2.6	R	Active	100	64	Gs	αs	-	59	-	Nanobody-35	CHEMBL449327	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW	10.1073/PNAS.2200155119	2022-06-29	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7EJ0	7EJ0_refined	3.2	R	Active	100	56	Gi/o	αo	-	61	-	scFv16	(-)-noradrenaline	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2022-04-13	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7SBF	7SBF_refined	2.9	R	Active	100	71	Gi/o	αi1	-	61	BRIL	scFv16	N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea	small-molecule	Agonist	-	-	Yes	No	Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P	10.1002/ANIE.202200269	2022-04-20	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7S15	7S15_refined	3.8	R	Active	93	83	-	-	-	-	-	-	2-[(4-{6-[(2,4-difluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA	10.1021/ACS.JMEDCHEM.1C01856	2022-06-08	Yes
GALR2	GAL₂	Galanin	A	Human	cryo-EM	7XJK	-	3.3	F	Active	100	72	Gq/11	αq	-	63	-	scFv16	Galanin, Human	peptide	Agonist	galanin-like peptide, spexin-1, galanin	peptide	Yes	No	Jiang W, Zheng S	10.1073/PNAS.2121465119	2022-06-29	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7EJ8	7EJ8_refined	3.0	R	Active	100	57	Gi/o	αo	-	61	-	scFv16	brimonidine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2022-04-13	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	7EZC	7EZC_refined	3.8	B	Active	74	70	-	-	-	-	BRIL	-	UK-432,097	small-molecule	Agonist	adenosine	small-molecule	Yes	No	Cui M, Zhou Q, Xu Y, Weng Y, Yao D, Zhao S, Song G	10.1107/S2052252522001907	2022-04-13	Yes
VIPR2	VPAC₂	VIP and PACAP	B1	Human	cryo-EM	7WBJ	7WBJ_refined	3.4	R	Active	100	82	Gs	αs	-	60	-	Nanobody-35	PACAP-27	peptide	Agonist	PACAP-27, secretin, GHRH, PACAP-38, VIP, PHI	peptide	No	No	Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW	10.1038/S41467-022-30041-Z	2022-05-18	Yes
5HT2A	5-HT_2A	5-Hydroxytryptamine	A	Human	cryo-EM	7RAN	-	3.5	A	Active	100	57	Gq/11	αq	Gi2-mini-Gq chimera	65	-	scFv16	3-[(3R)-3-methyl-1,2,3,6-tetrahydropyridin-1-ium-5-yl]-1H-pyrrolo[2,3-b]pyridine	small-molecule	Agonist	tryptamine, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-07-06	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7EJA	7EJA_refined	3.6	R	Active	100	58	Gi/o	αo	-	59	-	scFv16	dexmedetomidine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2022-04-13	Yes
AGRD1	ADGRD1	ADGRD	B2	Human	cryo-EM	7WU2	-	2.8	R	Active	100	32	Gs	αs	Mini-Gs	52	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B	10.1038/S41586-022-04580-W	2022-04-27	Yes
AGRG5	ADGRG5	ADGRG	B2	Human	cryo-EM	7EQ1	-	3.3	R	Active	100	54	Gs	αs	-	56	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	-	-	2022-05-11	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7WIG	7WIG_refined	2.7	R	Active	100	77	Gi/o	αi1	-	64	-	scFv16	~{N}-[(2~{R})-1-[[(1~{R},3~{S})-3-(aminomethyl)cyclohexyl]methylamino]-3-(1~{H}-indol-3-yl)-1-oxidanylidene-propan-2-yl]spiro[indene-1,4'-piperidine]-1'-carboxamide	small-molecule	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C	10.1038/S41422-022-00669-Z	2022-06-01	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7EJK	7EJK_refined	3.4	R	Active	100	55	Gi/o	αo	-	61	-	scFv16	oxymetazoline	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	-	-	2022-04-13	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7SCG	7SCG_refined	3.0	D	Active	100	71	Gi/o	αi1	-	61	-	scFv16	(2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide	small-molecule	Agonist	-	-	Yes	No	Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P	10.1002/ANIE.202200269	2022-04-20	Yes
BKRB2	B₂	Bradykinin	A	Human	cryo-EM	7F6I	-	2.8	A	Active	100	78	Gq/11	αq	-	63	-	-	kallidin	peptide	Agonist	[Hyp³]bradykinin, [des-Arg¹⁰]kallidin, Lys-[Hyp³]-bradykinin, kallidin, T-kinin, [des-Arg⁹]bradykinin, bradykinin	peptide	Yes	No	-	-	2022-01-05	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7X8S	7X8S_refined	3.1	R	Active	100	65	Gs	αs	-	60	-	Nanobody-35	2,4-bis(3-methoxy-4-thiophen-2-ylcarbonyloxy-phenyl)-1,3-bis[[4-(2-methylpropanoylamino)phenyl]carbonylamino]cyclobutane-1,3-dicarboxylic acid	small-molecule	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW	10.1073/PNAS.2200155119	2022-06-29	Yes
FPR1	FPR1	Formylpeptide	A	Human	cryo-EM	7WVU	7WVU_refined	3.3	R	Active	100	85	Gi/o	αi1	-	62	-	-	FME-LEU-PHE	peptide	Agonist	fMet-Leu-Phe, annexin I, spinorphin, cathepsin G	peptide	Yes	No	Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B	10.1038/S41467-022-29361-X	2022-04-13	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WU5	7WU5_refined	3.0	R	Active	100	31	Gi/o	αi1	Mini-Gi1	58	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B	10.1038/S41586-022-04580-W	2022-04-27	Yes
NPY4R	Y₄	Neuropeptide Y	A	Human	cryo-EM	7X9C	7X9C_refined	3.0	R	Active	100	81	Gi/o	αi1	-	61	-	-	Pancreatic polypeptide	peptide	Agonist	pancreatic polypeptide, PYY-(3-36), neuropeptide Y, peptide YY	peptide	Yes	No	Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B	10.1126/SCIADV.ABM1232	2022-05-18	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7WVV	7WVV_refined	2.9	R	Active	100	85	Gi/o	αi2	-	63	BRIL	-	synthetic peptide	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B	10.1038/S41467-022-29361-X	2022-04-13	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7VBH	7VBH_refined	3.0	R	Active	100	83	Gs	αs	-	53	-	Nanobody-35	Peptide 20	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW	10.1038/S41467-022-28683-0	2022-04-06	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7X2F	-	3.0	F	Active	100	63	Gs	αs	-	56	-	Nanobody-35	dopamine LY3154207	small-molecule small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S	10.1038/S41467-022-30929-W	2022-06-15	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7WVW	7WVW_refined	3.1	R	Active	100	85	Gi/o	αi2	-	63	BRIL	-	FME-TYR-PHE-ILE-ASN-ILE-LEU-THE-LEU	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B	10.1038/S41467-022-29361-X	2022-04-13	Yes
AGRL3	ADGRL3	ADGRL	B2	Human	cryo-EM	7SF7	-	2.9	A	Active	100	19	G12/13	α13	Gi2-mini-G13 chimera	54	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G	10.1038/S41586-022-04575-7	2022-04-27	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	cryo-EM	7V6A	-	3.6	R	Active	100	58	Gi/o	αi1	-	62	-	scFv16	methyl 4-[4-(3-methyl-2-oxidanylidene-benzimidazol-1-yl)piperidin-1-yl]piperidine-1-carboxylate	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	-	-	2022-05-11	Yes
NTR1	NTS₁	Neurotensin	A	Human	cryo-EM	7UL2	7UL2_refined	2.4	R	Inactive	3	69	-	-	-	-	-	Nanobody-6	meclinertant	small-molecule	Inverse agonist	large neuromedin N, neurotensin, neuromedin N, large neurotensin	peptide	Yes	No	-	-	2022-06-29	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7WVX	7WVX_refined	2.8	R	Active	100	85	Gi/o	αi2	-	61	BRIL	-	humanin	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B	10.1038/S41467-022-29361-X	2022-04-13	Yes
NMUR2	NMU2	Neuromedin U	A	Human	cryo-EM	7W57	-	3.2	R	Active	100	72	Gq/11	αq	-	59	-	scFv16	Neuromedin-S	peptide	Agonist	neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36	peptide	Yes	No	You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y	10.1038/S41467-022-29683-W	2022-04-20	Yes
FPR2	FPR2/ALX	Formylpeptide	A	Human	cryo-EM	7WVY	7WVY_refined	3.0	R	Active	100	85	Gi/o	αi2	-	63	BRIL	-	Amyloid beta-Peptide (1-42)	peptide	Agonist	LXA₄, fMet-Leu-Phe, LTD₄, PrP_106-126, aspirin triggered lipoxin A4, LL-37, serum amyloid A, humanin, 15-deoxy-LXA4, resolvin D1, aspirin-triggered resolvin D1, LTC₄, annexin I	peptide	Yes	No	Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B	10.1038/S41467-022-29361-X	2022-04-13	Yes
AGRD1	ADGRD1	ADGRD	B2	Human	cryo-EM	7EPT	-	3.0	R	Active	100	31	Gs	αs	-	53	-	Nanobody-35	-	-	-	-	-	No	No	Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP	10.1038/S41586-022-04619-Y	2022-05-11	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7F1O	-	3.1	F	Active	100	62	Gs	αs	-	60	-	Nanobody-35	dopamine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-06-15	Yes
5HT4R	5-HT₄	5-Hydroxytryptamine	A	Human	cryo-EM	7XT9	7XT9_refined	3.2	R	Active	100	76	Gs	αs	-	60	BRIL	-	5-hydroxytryptamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE	10.1016/J.MOLCEL.2022.05.031	2022-07-27	Yes
GALR1	GAL₁	Galanin	A	Human	cryo-EM	7WQ3	7WQ3_refined	2.7	R	Active	100	83	Gi/o	αi1	-	64	-	scFv16	galanin	peptide	Agonist	galanin-like peptide, galanin	peptide	Yes	No	-	-	2022-04-20	Yes
FPR1	FPR1	Formylpeptide	A	Human	cryo-EM	7EUO	7EUO_refined	2.9	R	Active	100	84	Gi/o	αi1	-	62	-	scFv16	Peptide Agonist fMLF	peptide	Agonist	fMet-Leu-Phe, annexin I, spinorphin, cathepsin G	peptide	Yes	No	-	-	2022-05-25	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7X2C	-	3.2	F	Active	100	63	Gs	αs	-	57	-	Nanobody-35	fenoldopam	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S	10.1038/S41467-022-30929-W	2022-06-29	Yes
GALR2	GAL₂	Galanin	A	Human	cryo-EM	7WQ4	7WQ4_refined	2.6	R	Active	100	73	Gq/11	αq	-	60	-	Nanobody-35	galanin	peptide	Agonist	galanin-like peptide, spexin-1, galanin	peptide	Yes	No	-	-	2022-04-20	Yes
OX2R	OX₂	Orexin	A	Human	cryo-EM	7SQO	7SQO_refined	3.2	R	Active	100	61	Gi/o	αi1	-	61	-	scFv16	methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate	small-molecule	Agonist	orexin-A, orexin-B	peptide	Yes	No	-	-	2022-05-25	Yes
GALR2	GAL₂	Galanin	A	Human	cryo-EM	7XJL	-	3.5	F	Active	100	72	Gq/11	αq	-	63	-	scFv16	Spexin	small-molecule	Agonist	galanin-like peptide, spexin-1, galanin	peptide	Yes	No	Jiang W, Zheng S	10.1073/PNAS.2121465119	2022-06-29	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7U2L	7U2L_refined	3.2	D	Active	100	71	Gi/o	αi1	-	61	-	scFv16	N-(5-carbamimidamidopentyl)-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide	small-molecule	Agonist	-	-	Yes	No	-	-	2022-05-04	Yes
OX2R	OX₂	Orexin	A	Human	cryo-EM	7SR8	-	3.3	R	Active	100	64	Gq/11	αq	-	63	-	scFv16	methyl (2R,3S)-3-[(methanesulfonyl)amino]-2-({[(1s,4S)-4-phenylcyclohexyl]oxy}methyl)piperidine-1-carboxylate	small-molecule	Agonist	orexin-A, orexin-B	peptide	Yes	No	Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM	10.1038/S41467-022-30601-3	2022-06-08	Yes
CNR1	CB₁	Cannabinoid	A	Human	X-ray	7FEE	7FEE_refined	2.7	A	Inactive	9	61	-	-	-	-	GlgA glycogen synthase	-	CP55940 6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole	small-molecule small-molecule	Agonist PAM	anandamide, 2-arachidonoylglycerol	small-molecule	No	No	Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S	10.1038/S41589-022-01038-Y	2022-06-15	Yes
S1PR2	S1P₂	Lysophospholipid (S1P)	A	Human	cryo-EM	7T6B	-	3.2	R	Active	100	75	G12/13	α13	-	60	-	scFv16	sphingosine 1-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	-	-	2022-04-06	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	cryo-EM	7V69	7V69_refined	3.4	R	Active	100	58	Gi/o	αi1	-	62	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	acetylcholine	small-molecule	Yes	No	-	-	2022-05-11	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7X2D	-	3.3	F	Active	100	63	Gs	αs	-	57	-	Nanobody-35	TAVAPADON	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S	10.1038/S41467-022-30929-W	2022-06-15	Yes
GP183	GPR183	A orphans	A	Human	cryo-EM	7TUY	7TUY_refined	3.0	R	Intermediate	42	73	-	-	-	-	BRIL	anti-BRIL Fab heavy chain anti-BRIL Fab light chain anti-Fab Nanobody	8-[(2E)-3-(4-chlorophenyl)prop-2-enoyl]-3-[(3,4-dichlorophenyl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one	small-molecule	Inverse agonist	7β, 27-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7α,25-dihydroxycholesterol, 7α-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 25-hydroxycholesterol, 27-hydroxycholesterol	small-molecule	No	No	-	-	2022-04-13	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7WUQ	-	2.9	R	Active	100	28	Gs	αs	-	55	-	Nanobody-35	-	-	-	-	-	No	No	Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X	10.1038/S41586-022-04590-8	2022-04-27	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7F0T	-	3.1	F	Active	100	63	Gs	αs	-	58	-	Nanobody-35	dopamine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-06-15	Yes
5HT4R	5-HT₄	5-Hydroxytryptamine	A	Human	cryo-EM	7XT8	-	3.1	R	Active	100	76	Gs	αs	-	60	BRIL	Nanobody-35	5-hydroxytryptamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE	10.1016/J.MOLCEL.2022.05.031	2022-07-27	Yes
GP183	GPR183	A orphans	A	Human	cryo-EM	7TUZ	7TUZ_refined	3.1	R	Active	100	79	Gi/o	αi1	-	64	-	scFv16	(2S,4aS,4bS,7R,8S,8aS,9R,10aR)-7-[(2R,3R)-7-hydroxy-3,7-dimethyloctan-2-yl]-4a,7,8-trimethyltetradecahydrophenanthrene-2,9-diol	small-molecule	Agonist	7β, 27-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7α,25-dihydroxycholesterol, 7α-hydroxycholesterol, 7β-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 25-hydroxycholesterol, 27-hydroxycholesterol	small-molecule	No	No	-	-	2022-04-13	Yes
BKRB2	B₂	Bradykinin	A	Human	cryo-EM	7F6H	-	2.9	A	Active	100	78	Gq/11	αq	-	63	-	-	bradykinin	peptide	Agonist	[Hyp³]bradykinin, [des-Arg¹⁰]kallidin, Lys-[Hyp³]-bradykinin, kallidin, T-kinin, [des-Arg⁹]bradykinin, bradykinin	peptide	Yes	No	-	-	2022-01-05	Yes
SMO	SMO	Frizzled	F	Human	X-ray	7ZI0	7ZI0_refined	3.0	A	Inactive	4	61	-	-	-	-	BRIL	-	3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide	small-molecule	Antagonist	-	-	No	No	Kinnebrew M, Woolley RE, Ansell TB, Byrne EFX, Frigui S, Luchetti G, Sircar R, Nachtergaele S, Mydock-McGrane L, Krishnan K, Newstead S, Sansom MSP, Covey DF, Siebold C, Rohatgi R	10.1126/SCIADV.ABM5563	2022-06-15	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7RA3	7RA3_refined	3.2	R	Active	100	80	Gs	αs	Engineered G alpha	56	-	scFv16 Nanobody-35	gastric inhibitory polypeptide (human) - Incretin	peptide	Agonist	gastric inhibitory polypeptide	peptide	No	No	Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW	10.1073/PNAS.2116506119	2022-04-13	Yes
GIPR	GIP	Glucagon	B1	Human	cryo-EM	7RBT	-	3.1	R	Active	100	81	Gs	αs	-	54	-	scFv16 Nanobody-35	tirzepatide 2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol	peptide small-molecule	Agonist PAM	gastric inhibitory polypeptide	peptide	No	No	Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW	10.1073/PNAS.2116506119	2022-04-13	Yes
CNR1	CB₁	Cannabinoid	A	Human	cryo-EM	7WV9	7WV9_refined	3.4	R	Active	100	61	Gi/o	αi2	-	63	-	scFv16	CP55940 6-methyl-3-[(1S)-2-nitro-1-thiophen-2-yl-ethyl]-2-phenyl-1H-indole	small-molecule small-molecule	Agonist PAM	anandamide, 2-arachidonoylglycerol	small-molecule	Yes	No	Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S	10.1038/S41589-022-01038-Y	2022-06-15	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7RG9	-	3.2	R	Active	100	58	Gs	αs	-	54	-	scFv16 Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW	10.1073/PNAS.2116506119	2022-04-13	Yes
NPY2R	Y₂	Neuropeptide Y	A	Human	cryo-EM	7X9B	7X9B_refined	3.4	R	Active	100	79	Gi/o	αi1	-	62	-	-	neuropeptide Y	peptide	Agonist	neuropeptide Y-(3-36), PYY-(3-36), neuropeptide Y, peptide YY, pancreatic polypeptide	peptide	Yes	No	Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B	10.1126/SCIADV.ABM1232	2022-05-18	Yes
GLP1R	GLP-1	Glucagon	B1	Human	cryo-EM	7RGP	-	2.9	R	Active	100	82	Gs	αs	Engineered G alpha	53	-	scFv16 Nanobody-35	tirzepatide	peptide	Agonist	glucagon-like peptide 1-(7-37), glucagon-like peptide 1-(7-36) amide, glucagon	peptide	No	No	Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW	10.1073/PNAS.2116506119	2022-04-13	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7UL4	7UL4_refined	2.8	A	Inactive	3	72	-	-	-	-	-	Megabody-6	alvimopan	small-molecule	Antagonist	-	-	Yes	No	-	-	2022-06-29	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WU3	-	3.1	R	Active	100	31	Gs	αs	Mini-Gs	52	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B	10.1038/S41586-022-04580-W	2022-04-27	Yes
VIPR2	VPAC₂	VIP and PACAP	B1	Human	cryo-EM	7VQX	7VQX_refined	2.7	R	Active	100	82	Gs	αs	-	60	-	Nanobody-35	PACAP-27	peptide	Agonist	PACAP-27, secretin, GHRH, PACAP-38, VIP, PHI	peptide	No	No	Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW	10.1038/S41467-022-30041-Z	2022-05-18	Yes
5HT5A	5-HT_5A	5-Hydroxytryptamine	A	Human	cryo-EM	7UM5	-	2.7	A	Active	100	75	Gi/o	αo	Mini-Go	58	-	scFv16	5-CT	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL	10.1038/S41594-022-00796-6	2022-07-20	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WU4	7WU4_refined	3.4	R	Active	100	31	Gi/o	αi1	Mini-Gi1	58	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B	10.1038/S41586-022-04580-W	2022-04-27	Yes
ADRB3	β₃	Adrenoceptors	A	Dog	cryo-EM	7XJI	7XJI_refined	3.9	R	Active	100	68	Gs	αs	-	59	-	Nanobody-35	3-[3-[2-[[(2~{S})-2-(3-chlorophenyl)-2-oxidanyl-ethyl]amino]ethylamino]phenyl]benzoic acid	small-molecule	Agonist	-	-	Yes	No	Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O	10.1016/J.BBRC.2022.04.065	2022-05-04	Yes
TRFR	TRH₁	Thyrotropin-releasing hormone	A	Human	cryo-EM	7WKD	7WKD_refined	3.0	R	Active	100	66	Gq/11	αq	-	60	-	scFv16	TRH	peptide	Agonist	TRH	peptide	Yes	No	Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE	10.1038/S41422-022-00641-X	2022-06-15	Yes
AGRG1	ADGRG1	ADGRG	B2	Human	cryo-EM	7SF8	-	2.7	A	Active	100	37	G12/13	α13	Gi2-mini-G13 chimera	53	-	-	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G	10.1038/S41586-022-04575-7	2022-04-27	Yes
NPY1R	Y₁	Neuropeptide Y	A	Human	cryo-EM	7X9A	7X9A_refined	3.2	R	Active	100	80	Gi/o	αi1	-	61	-	-	neuropeptide Y	peptide	Agonist	pancreatic polypeptide, neuropeptide Y, peptide YY	peptide	Yes	No	Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B	10.1126/SCIADV.ABM1232	2022-05-18	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7WUI	-	3.1	R	Active	100	24	Gs	αs	Mini-Gs	55	-	-	IP15	peptide	Agonist	-	-	No	No	Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X	10.1038/S41586-022-04590-8	2022-04-27	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7F24	-	4.2	F	Active	100	62	Gs	αs	-	57	-	-	dopamine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-06-15	Yes
AGRG4	ADGRG4	ADGRG	B2	Human	cryo-EM	7WUJ	-	3.3	E	Active	100	9	Gs	αs	Mini-Gs	55	-	scFv16 Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X	10.1038/S41586-022-04590-8	2022-04-27	Yes
ADRB3	β₃	Adrenoceptors	A	Dog	cryo-EM	7XJH	7XJH_refined	3.3	R	Active	100	68	Gs	αs	-	59	-	Nanobody-35	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	-	-	2022-05-04	Yes
HRH2	H₂	Histamine	A	Human	cryo-EM	7UL3	7UL3_refined	3.0	A	Inactive	3	75	-	-	-	-	-	Nanobody-6M NabFab HC NabFab LC	famotidine	small-molecule	Antagonist	histamine	small-molecule	Yes	No	-	-	2022-06-29	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	7S0G	-	3.9	R	Active	100	57	Gs	αs	Gi1-Gs chimera	56	-	-	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY	10.1038/S41594-021-00679-2	2021-11-17	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7F1Z	-	3.5	F	Active	100	62	Gs	αs	-	60	-	-	dopamine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-06-15	Yes
5HT4R	5-HT₄	5-Hydroxytryptamine	A	Human	cryo-EM	7XTA	7XTA_refined	3.2	R	Active	100	73	Gi/o	αi1	-	62	BRIL	scFv16	5-hydroxytryptamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE	10.1016/J.MOLCEL.2022.05.031	2022-07-27	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	7S0F	-	3.0	R	Active	100	56	Gi/o	αi1	-	63	-	-	LEVISOPRENALINE	small-molecule	Agonist	-	-	Yes	No	Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY	10.1038/S41594-021-00679-2	2021-11-17	Yes
DRD1	D₁	Dopamine	A	Human	cryo-EM	7F23	-	3.6	F	Active	100	62	Gs	αs	-	60	-	Nanobody-35	dopamine	small-molecule	Agonist	(-)-noradrenaline, noradrenaline, dopamine, L-NOREPINEPHRINE, 5-hydroxytryptamine	small-molecule	Yes	No	-	-	2022-06-15	Yes
NMUR1	NMU1	Neuromedin U	A	Human	cryo-EM	7W53	-	3.2	R	Active	100	62	Gq/11	αq	-	54	-	scFv16	Neuromedin U-25 (human)	peptide	Agonist	neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36	peptide	Yes	No	You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y	10.1038/S41467-022-29683-W	2022-04-20	Yes
5HT5A	5-HT_5A	5-Hydroxytryptamine	A	Human	X-ray	7UM4	7UM4_refined	2.8	A	Inactive	34	71	-	-	-	-	PGS	-	CHEMBL3654198	small-molecule	Antagonist	5-hydroxytryptamine	small-molecule	No	No	Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL	10.1038/S41594-022-00796-6	2022-07-20	Yes
NMUR2	NMU2	Neuromedin U	A	Human	cryo-EM	7W55	-	2.8	R	Active	100	73	Gq/11	αq	-	60	-	scFv16	Neuromedin U-25 (human)	peptide	Agonist	neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36	peptide	Yes	No	You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y	10.1038/S41467-022-29683-W	2022-04-20	Yes
NMUR1	NMU1	Neuromedin U	A	Human	cryo-EM	7W56	-	2.9	R	Active	100	65	Gq/11	αq	-	59	-	scFv16	Neuromedin-S	peptide	Agonist	neuromedin S-33, neuromedin U-23, neuromedin U-25, neuromedin S-36	peptide	Yes	No	You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y	10.1038/S41467-022-29683-W	2022-04-20	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	cryo-EM	7V68	-	3.4	R	Active	100	58	Gi/o	αi1	-	62	-	scFv16	iperoxo LY2119620	small-molecule small-molecule	Agonist PAM	acetylcholine	small-molecule	Yes	No	-	-	2022-05-11	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7UL5	-	3.1	A	Inactive	3	77	-	-	-	-	-	Nanobody-6	Apo (no ligand)	none	Apo (no ligand)	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	-	-	2022-06-29	Yes
5HT5A	5-HT_5A	5-Hydroxytryptamine	A	Human	cryo-EM	7UM6	-	2.8	A	Active	100	72	Gi/o	αo	Mini-Go	58	-	scFv16	lisuride	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL	10.1038/S41594-022-00796-6	2022-07-20	Yes
5HT5A	5-HT_5A	5-Hydroxytryptamine	A	Human	cryo-EM	7UM7	-	2.8	A	Active	100	72	Gi/o	αo	Mini-Go	58	-	scFv16	methylergonovine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL	10.1038/S41594-022-00796-6	2022-07-20	Yes
5HT6R	5-HT₆	5-Hydroxytryptamine	A	Human	cryo-EM	7XTB	7XTB_refined	3.3	R	Active	100	63	Gs	αs	-	60	BRIL	Nanobody-35	5-hydroxytryptamine	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE	10.1016/J.MOLCEL.2022.05.031	2022-07-27	Yes
5HT7R	5-HT₇	5-Hydroxytryptamine	A	Human	cryo-EM	7XTC	7XTC_refined	3.2	R	Active	100	57	Gs	αs	-	61	BRIL	Nanobody-35	5-CT	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE	10.1016/J.MOLCEL.2022.05.031	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	X-ray	7SUS	7SUS_refined	2.7	A	Inactive	3	76	-	-	-	-	Rubredoxin	-	(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide	small-molecule	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	cryo-EM	7W0L	7W0L_refined	3.6	R	Active	100	78	Gi/o	αi1	-	64	BRIL	scFv16	(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide	small-molecule	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	cryo-EM	7W0M	7W0M_refined	3.7	R	Active	100	76	Gi/o	αi1	-	62	BRIL	scFv16	(1R,2S)-N-[4-(2,6-dimethoxyphenyl)-5-(6-methylpyridin-2-yl)-1,2,4-triazol-3-yl]-1-(5-methylpyrimidin-2-yl)-1-oxidanyl-propane-2-sulfonamide	small-molecule	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	cryo-EM	7W0N	-	4.2	R	Active	100	78	Gi/o	αi1	-	64	BRIL	scFv16	apelin receptor early endogenous ligand	peptide	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	cryo-EM	7W0O	7W0O_refined	3.8	R	Active	100	77	Gi/o	αi1	-	64	BRIL	scFv16	apelin receptor early endogenous ligand	peptide	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
APJ	apelin	Apelin	A	Human	cryo-EM	7W0P	7W0P_refined	3.2	R	Active	100	77	Gi/o	αi1	-	64	BRIL	scFv16	apelin receptor early endogenous ligand	peptide	Agonist	apelin-36, [Pyr¹]apelin-13, Elabela/Toddler-11, apelin-13, Elabela/Toddler-21, apelin-17, apelin receptor early endogenous ligand, Elabela/Toddler-32	peptide	Yes	No	Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F	10.1038/S41594-022-00797-5	2022-07-27	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7XOU	7XOU_refined	3.2	R	Active	100	67	Gs	αs	-	58	-	Nanobody-35	CCK-8	peptide	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM	10.1038/S41421-022-00420-3	2022-07-20	Yes
CCKAR	CCK₁	Cholecystokinin	A	Human	cryo-EM	7XOV	7XOV_refined	3.0	R	Active	100	67	Gs	αs	-	58	-	Nanobody-35	SR146131	small-molecule	Agonist	CCK-4, gastrin-17, desulfated cholecystokinin-8, CCK-33, CCK-58, CCK-39, CCK-8	peptide	Yes	No	Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM	10.1038/S41421-022-00420-3	2022-07-20	Yes
GASR	CCK₂	Cholecystokinin	A	Human	cryo-EM	7XOW	7XOW_refined	3.1	R	Active	100	62	Gq/11	αq	-	61	-	scFv16	desulfated gastrin-17	peptide	Agonist	CCK-4, gastrin-17, gastrin-71, desulfated cholecystokinin-8, desulfated gastrin-34, desulfated gastrin-71, gastrin-14, desulfated gastrin-14, CCK-33, gastrin-34, CCK-58, CCK-39, CCK-8, desulfated gastrin-17	peptide	Yes	No	Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM	10.1038/S41421-022-00420-3	2022-07-20	Yes
GASR	CCK₂	Cholecystokinin	A	Human	cryo-EM	7XOX	7XOX_refined	3.1	R	Active	100	62	Gq/11	αq	-	61	-	scFv16	CCK-8	peptide	Agonist	CCK-4, gastrin-17, gastrin-71, desulfated cholecystokinin-8, desulfated gastrin-34, desulfated gastrin-71, gastrin-14, desulfated gastrin-14, CCK-33, gastrin-34, CCK-58, CCK-39, CCK-8, desulfated gastrin-17	peptide	Yes	No	Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM	10.1038/S41421-022-00420-3	2022-07-20	Yes
GALR2	GAL₂	Galanin	A	Human	cryo-EM	7XBD	-	3.1	A	Active	100	72	Gq/11	αq	-	64	-	scFv16	Galanin, Human	peptide	Agonist	galanin-like peptide, spexin-1, galanin	peptide	Yes	No	Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY	10.1371/JOURNAL.PBIO.3001714	2022-07-13	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7WJ5	7WJ5_refined	3.7	R	Active	100	76	Gi/o	αi1	-	60	BRIL	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W	10.7554/ELIFE.76823	2022-07-13	Yes
CX3C1	CX₃CR1	Chemokine	A	Human	cryo-EM	7XBW	7XBW_refined	2.8	R	Active	16	81	Gi/o	αi1	-	61	-	-	Apo (no ligand)	none	Apo (no ligand)	CX₃CL1	peptide	Yes	No	Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q	10.1126/SCIADV.ABN8048	2022-07-13	Yes
CX3C1	CX₃CR1	Chemokine	A	Human	cryo-EM	7XBX	7XBX_refined	3.4	R	Active	16	81	Gi/o	αi1	-	60	-	-	CX3CL1	peptide	Agonist	CX₃CL1	peptide	Yes	No	-	-	2022-07-13	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK3	7SK3_refined	3.8	A	Active	94	84	-	-	-	-	-	CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain	CXCL12α	peptide	Agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK4	-	3.3	A	Active	94	84	-	-	-	-	-	CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain	Stromal cell-derived factor 1	peptide	Agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK5	7SK5_refined	4.0	A	Active	94	83	-	-	-	-	-	CID24 Fab heavy chain CID24 Fab light chain anti-Fab Nanobody	Stromal cell-derived factor 1	peptide	Agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK6	7SK6_refined	4.0	A	Active	94	83	-	-	-	-	-	CID24 Fab light chain CID24 Fab heavy chain	Stromal cell-derived factor 1	peptide	Agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK7	-	3.3	A	Active	94	74	-	-	-	-	-	CID25 Fab light chain CID25 Fab heavy chain anti-Fab Nanobody	Stromal cell-derived factor 1 (1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium	peptide small-molecule	Agonist Partial agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
GPBAR	GPBA	Bile acid	A	Human	cryo-EM	7XTQ	7XTQ_refined	3.2	R	Active	100	83	Gs	αs	-	58	-	Nanobody-35	CHEMBL2181246	small-molecule	Agonist	lithocholic acid, chenodeoxycholic acid, cholic acid, deoxycholic acid	small-molecule	No	No	Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P	10.1073/PNAS.2117054119	2022-07-06	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK9	7SK9_refined	3.7	A	Active	94	78	-	-	-	-	-	CID24 Fab heavy chain CID24 Fab light chain	(1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium	small-molecule	Partial agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
ACKR3	ACKR3	Chemokine	A	Human	cryo-EM	7SK8	7SK8_refined	3.3	A	Active	94	85	-	-	-	-	-	CID25 Fab light chain CID25 Fab heavy chain CID24 Fab light chain CID24 Fab heavy chain	Stromal cell-derived factor 1 (1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium	peptide small-molecule	Agonist Partial agonist	CXCL12α, CXCL11	peptide	Yes	No	Yen YC, Schafer CT, Gustavsson M, Eberle SA, Dominik PK, Deneka D, Zhang P, Schall TJ, Kossiakoff AA, Tesmer JJG, Handel TM	10.1126/SCIADV.ABN8063	2022-07-27	Yes
MRGRD	MRGPRD	A orphans	A	Human	cryo-EM	7Y12	7Y12_refined	3.1	R	Active	100	82	Gi/o	αi1	-	62	BRIL	scFv16	β-alanine	small-molecule	Agonist	β-alanine	small-molecule	No	No	-	-	2022-07-20	Yes
MRGRD	MRGPRD	A orphans	A	Human	cryo-EM	7Y13	-	3.1	R	Active	58	82	-	-	-	-	BRIL	-	Apo (no ligand)	none	Apo (no ligand)	β-alanine	small-molecule	No	No	-	-	2022-07-20	Yes
MRGRD	MRGPRD	A orphans	A	Human	cryo-EM	7Y14	7Y14_refined	3.2	R	Active	58	82	-	-	-	-	BRIL	-	β-alanine	small-molecule	Agonist	β-alanine	small-molecule	No	No	-	-	2022-07-20	Yes
MRGRD	MRGPRD	A orphans	A	Human	cryo-EM	7Y15	7Y15_refined	2.9	R	Active	100	82	Gi/o	αi1	-	62	BRIL	scFv16	Apo (no ligand)	none	Apo (no ligand)	β-alanine	small-molecule	No	No	-	-	2022-07-20	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	8DCR	-	2.6	R	Active	100	57	Gs	αs	-	51	T4-Lysozyme	Nanobody-35	Dobutamine	small-molecule	Agonist	-	-	Yes	No	Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY	10.1038/S41467-022-31823-1	2022-07-27	Yes
ADRB1	β₁	Adrenoceptors	A	Wild turkey	cryo-EM	8DCS	8DCS_refined	2.5	R	Active	100	57	Gs	αs	-	51	T4-Lysozyme	Nanobody-35	4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile	small-molecule	Agonist	-	-	Yes	No	Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY	10.1038/S41467-022-31823-1	2022-07-27	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	cryo-EM	8DPF	-	2.8	A	Active	100	58	Gq/11	αq	Gi2-mini-Gq chimera	62	-	scFv16	lorcaserin	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Gumpper RH, Fay JF, Roth BL	10.1016/J.CELREP.2022.111211	2022-08-24	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	cryo-EM	8DPG	-	3.6	A	Active	100	58	Gq/11	αq	Gi2-mini-Gq chimera	62	-	scFv16	psilocin	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Gumpper RH, Fay JF, Roth BL	10.1016/J.CELREP.2022.111211	2022-08-24	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	cryo-EM	8DPH	-	3.2	A	Active	100	58	Gq/11	αq	Gi2-mini-Gq chimera	62	-	scFv16	lorcaserin	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Gumpper RH, Fay JF, Roth BL	10.1016/J.CELREP.2022.111211	2022-08-24	Yes
5HT2C	5-HT_2C	5-Hydroxytryptamine	A	Human	cryo-EM	8DPI	-	3.4	A	Active	100	58	Gq/11	αq	Gi2-mini-Gq chimera	62	-	scFv16	lorcaserin	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Gumpper RH, Fay JF, Roth BL	10.1016/J.CELREP.2022.111211	2022-08-24	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7XAT	7XAT_refined	2.9	A	Active	100	78	Gi/o	αi1	-	63	-	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C	10.1038/S41421-022-00405-2	2022-08-31	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7XAU	7XAU_refined	3.0	A	Active	100	76	Gi/o	αi1	-	63	-	scFv16	Octreotide	peptide	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C	10.1038/S41421-022-00405-2	2022-08-31	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7XAV	7XAV_refined	2.9	A	Active	100	76	Gi/o	αi1	-	63	-	scFv16	lanreotide	peptide	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C	10.1038/S41421-022-00405-2	2022-08-31	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7XMR	7XMR_refined	3.1	R	Active	100	77	Gi/o	αi1	-	63	-	-	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q	10.1038/S41422-022-00679-X	2022-08-03	Yes
SSR2	SST2	Somatostatin	A	Human	X-ray	7XN9	7XN9_refined	2.6	A	Inactive	3	79	-	-	-	-	-	-	L-054,522	small-molecule	Antagonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q	10.1038/S41422-022-00679-X	2022-08-03	Yes
SSR2	SST2	Somatostatin	A	Human	X-ray	7XNA	-	2.7	A	Inactive	3	78	-	-	-	-	-	-	CYN 154806	peptide	Antagonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	No	No	Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q	10.1038/S41422-022-00679-X	2022-08-03	Yes
SSR4	SST4	Somatostatin	A	Human	cryo-EM	7XMS	7XMS_refined	2.9	R	Active	100	71	Gi/o	αi1	-	63	-	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q	10.1038/S41422-022-00679-X	2022-08-03	Yes
SSR4	SST4	Somatostatin	A	Human	cryo-EM	7XMT	7XMT_refined	2.8	R	Active	100	68	Gi/o	αi1	-	63	-	scFv16	J-2156	small-molecule	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q	10.1038/S41422-022-00679-X	2022-08-03	Yes
TRFR	TRH₁	Thyrotropin-releasing hormone	A	Human	cryo-EM	7X1T	-	3.3	A	Active	100	68	Gq/11	αq	-	61	-	scFv16	taltirelin	small-molecule	Agonist	TRH	peptide	Yes	No	Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C	10.1038/S41422-022-00646-6	2022-08-31	Yes
TRFR	TRH₁	Thyrotropin-releasing hormone	A	Human	cryo-EM	7X1U	-	3.2	A	Active	100	68	Gq/11	αq	-	62	-	scFv16	TRH	peptide	Agonist	TRH	peptide	Yes	No	Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C	10.1038/S41422-022-00646-6	2022-08-31	Yes
OXYR	OT	Vasopressin and oxytocin	A	Human	cryo-EM	7QVM	7QVM_refined	3.3	R	Active	100	64	Gi/o	αo	-	59	-	scFv16	oxytocin	peptide	Agonist	oxytocin, vasopressin	peptide	Yes	No	Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A	10.1038/S41467-022-31325-0	2022-08-10	Yes
CCR2	CCR2	Chemokine	A	Human	cryo-EM	7XA3	7XA3_refined	2.9	R	Active	100	79	Gi/o	αi1	-	65	-	scFv16	C-C motif chemokine 2	peptide	Agonist	CCL24, CCL2, CCL26, CCL8, CCL13, CCL7, CCL16, CCL11	peptide	No	No	Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H	10.1038/S41421-022-00403-4	2022-08-24	Yes
CCR3	CCR3	Chemokine	A	Human	cryo-EM	7X9Y	7X9Y_refined	3.1	R	Active	100	83	Gi/o	αi1	-	62	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	CCL24, CCL5, CCL2, CCL28, CXCL9, CCL26, CCL13, CCL8, CCL7, CCL15, CXCL10, CXCL11, CCL11	peptide	No	No	Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H	10.1038/S41421-022-00403-4	2022-08-24	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7XW5	-	3.0	R	Active	100	75	Gs	αs	-	59	-	Nanobody-35	Glycoprotein hormones alpha chain Thyrotropin subunit beta N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide	protein protein small-molecule	Agonist	TSH	peptide	Yes	No	Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE	10.1038/S41586-022-05173-3	2022-08-24	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7XW6	-	2.8	R	Active	100	74	Gs	αs	-	57	-	Nanobody-35	M22 antibody light chain M22 antibody heavy chain N-[4-[[5-[(2S)-3-benzyl-5-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide	protein protein small-molecule	Agonist	TSH	peptide	Yes	No	Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE	10.1038/S41586-022-05173-3	2022-08-17	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7XW7	-	5.5	R	Inactive	14	74	-	-	-	-	-	-	K1-70 scFv heavy chain K1-70 scFv light chain	protein protein	Antagonist	TSH	peptide	Yes	No	Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE	10.1038/S41586-022-05173-3	2022-08-17	Yes
S1PR5	S1P₅	Lysophospholipid (S1P)	A	Human	X-ray	7YXA	7YXA_refined	2.2	A	Inactive	9	72	-	-	-	-	BRIL	-	4-[6-(2-naphthalen-1-ylethoxy)-2,3,4,5-tetrahydro-1H-3-benzazepin-3-ium-3-yl]butanoic acid	small-molecule	Antagonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	-	-	2022-08-10	Yes
PE2R3	EP₃	Prostanoid	A	Human	cryo-EM	7WU9	7WU9_refined	3.4	R	Active	100	70	Gi/o	αi1	-	38	-	scFv16	-	-	-	PGD₂, PGE₁, thromboxane A₂, PGE₂, PGF_2α, PGI₂	small-molecule	Yes	No	-	-	2022-08-17	Yes
AA2AR	A_2A	Adenosine	A	Human	cryo-EM	7T32	7T32_refined	3.4	A	Inactive	1	69	-	-	-	-	BRIL	-	ZM-241385	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Zhang K, Wu H, Hoppe N, Manglik A, Cheng Y	10.1038/S41467-022-32125-2	2022-08-10	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	8CU6	8CU6_refined	2.8	A	Inactive	1	72	-	-	-	-	BRIL	-	LJ-4517	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Shiriaeva A, Park D, Kim G, Lee Y, Hou X, Jarhad DB, Kim G, Yu J, Hyun YE, Kim W, Gao ZG, Jacobson KA, Han GW, Stevens RC, Jeong LS, Choi S, Cherezov V	10.1021/ACS.JMEDCHEM.2C00462	2022-08-31	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	8CU7	-	2.1	A	Inactive	1	72	-	-	-	-	BRIL	-	LJ-4517	small-molecule	Antagonist	adenosine	small-molecule	Yes	Yes	-	-	2022-08-31	Yes
AA2AR	A_2A	Adenosine	A	Human	X-ray	8DU3	8DU3_refined	2.5	A	Inactive	1	72	-	-	-	-	BRIL	-	(4M)-6-bromo-4-(furan-2-yl)quinazolin-2-amine	small-molecule	Antagonist	adenosine	small-molecule	Yes	No	Bolteau R, Duroux R, Laversin A, Vreulz B, Shiriaeva A, Stauch B, Han GW, Cherezov V, Renault N, Barczyk A, Ravez S, Coevoet M, Melnyk P, Liberelle M, Yous S	10.1016/J.EJMECH.2022.114620	2022-08-10	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVJ	-	3.2	R	Active	100	62	Gs	αs	-	59	-	Nanobody-35	PTHrP[1-36]	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVK	7VVK_refined	3.3	R	Active	100	56	Gs	αs	-	58	-	Nanobody-35	teriparatide	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVL	-	2.8	R	Active	100	58	Gs	αs	-	58	-	Nanobody-35	teriparatide	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVM	-	3.2	R	Active	100	60	Gs	αs	-	58	-	Nanobody-35	Parathyroid hormone	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVN	-	3.8	R	Active	100	51	Gs	αs	-	58	-	Nanobody-35	teriparatide	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	7VVO	-	4.1	R	Active	100	51	Gs	αs	-	58	-	Nanobody-35	Parathyroid hormone	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	-	-	2022-08-03	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7XKD	-	2.4	R	Active	100	26	Gs	αs	-	57	-	Nanobody-35	PRASTERONE	small-molecule	Agonist	-	-	No	No	-	-	2022-08-10	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7XKE	7XKE_refined	2.9	R	Active	100	25	Gs	αs	Mini-Gs	60	-	Nanobody-35	PRASTERONE	small-molecule	Agonist	-	-	No	No	-	-	2022-08-10	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7XKF	-	2.4	R	Active	100	26	Gs	αs	-	57	-	Nanobody-35	PRASTERONE	small-molecule	Agonist	-	-	No	No	-	-	2022-08-10	Yes
AGRG2	ADGRG2	ADGRG	B2	Mouse	cryo-EM	7YP7	7YP7_refined	3.1	R	Active	100	24	Gs	αs	-	59	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	-	-	2022-08-24	Yes
SMO	SMO	Frizzled	F	Mouse	cryo-EM	8CXO	8CXO_refined	3.7	A	Inactive	15	43	-	-	-	-	GlgA glycogen synthase	-	Cholesterol	small-molecule	Agonist	-	-	No	No	Zhang K, Wu H, Hoppe N, Manglik A, Cheng Y	10.1038/S41467-022-32125-2	2022-08-03	Yes
GP119	GPR119	GPR18, GPR55 and GPR119	A	Human	cryo-EM	7XZ5	-	3.1	R	Active	100	87	Gs	αs	-	58	BRIL	Nanobody-35	(4R,7R,18E)-4,7-dihydroxy-N,N,N-trimethyl-10-oxo-3,5,9-trioxa-4-phosphaheptacos-18-en-1-aminium 4-oxide	small-molecule	Agonist	anandamide, N-oleoylethanolamide, SEA, N-palmitoylethanolamine	small-molecule	Yes	No	Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE	10.1038/S41594-022-00816-5	2022-08-24	Yes
GP119	GPR119	GPR18, GPR55 and GPR119	A	Human	cryo-EM	7XZ6	-	2.8	R	Active	100	87	Gs	αs	-	58	BRIL	Nanobody-35	APD668	small-molecule	Agonist	anandamide, N-oleoylethanolamide, SEA, N-palmitoylethanolamine	small-molecule	Yes	No	Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE	10.1038/S41594-022-00816-5	2022-08-24	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7T9I	-	2.9	R	Active	100	78	Gs	αs	Mini-Gs	56	-	Nanobody-35	Glycoprotein hormones alpha chain Thyrotropin subunit beta	protein protein	Agonist	TSH	peptide	Yes	No	Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A	10.1038/S41586-022-05159-1	2022-08-03	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7T9M	-	3.1	R	Inactive	31	74	-	-	-	-	-	-	CS-17 heavy chain CS-17 light chain	protein protein	Inverse agonist	TSH	peptide	Yes	No	Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A	10.1038/S41586-022-05159-1	2022-08-10	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7T9N	-	2.9	R	Active	100	73	Gs	αs	Mini-Gs	56	-	M22 Fab light chain M22 Fab heavy chain Nanobody-35	M22 antibody light chain M22 antibody heavy chain	protein protein	Agonist	TSH	peptide	Yes	No	Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A	10.1038/S41586-022-05159-1	2022-08-03	Yes
TSHR	TSH	Glycoprotein hormone	A	Human	cryo-EM	7UTZ	-	2.4	R	Active	100	79	Gs	αs	Mini-Gs	56	-	Nanobody-35	Glycoprotein hormones alpha chain analog TR1402 Thyrotropin subunit beta	protein protein	Agonist	TSH	peptide	Yes	No	Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A	10.1038/S41586-022-05159-1	2022-08-03	Yes
HRH3	H₃	Histamine	A	Human	X-ray	7F61	7F61_refined	2.6	A	Inactive	8	68	-	-	-	-	BRIL	-	N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide	small-molecule	Antagonist	histamine	small-molecule	No	No	Peng X, Yang L, Liu Z, Lou S, Mei S, Li M, Chen Z, Zhang H	10.1038/S41467-022-33880-Y	2022-10-26	Yes
P2Y12	P2Y₁₂	P2Y	A	Human	Unknown	7PP1	-	2.8	A	Intermediate	42	78	-	-	-	-	BRIL	-	selatogrel	small-molecule	Antagonist	ATP, ADP	small-molecule	Yes	No	Pons V, Garcia C, Tidten-Luksch N, Mac Sweeney A, Caroff E, Gales C, Riederer MA	10.1016/j.bcp.2022.115291	2022-11-02	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	cryo-EM	7SRQ	7SRQ_refined	2.7	R	Intermediate	42	53	-	-	-	-	-	-	Lysergide	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL	10.1016/J.NEURON.2022.08.006	2022-09-21	Yes
V2R	V₂	Vasopressin and oxytocin	A	Human	cryo-EM	7R0C	-	4.7	A	Active	100	76	Beta	Beta-arrestin-1	-	84	-	scFv30	-	-	-	oxytocin, vasopressin	peptide	Yes	No	Bous J, Fouillen A, Orcel H, Trapani S, Cong X, Fontanel S, Saint-Paul J, Lai-Kee-Him J, Urbach S, Sibille N, Sounier R, Granier S, Mouillac B, Bron P	10.1126/SCIADV.ABO7761	2022-09-14	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	cryo-EM	7SRR	-	2.9	R	Active	100	57	Gq/11	αq	Gi2-mini-Gq chimera	63	-	scFv16	Lysergide	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL	10.1016/J.NEURON.2022.08.006	2022-09-21	Yes
5HT2B	5-HT_2B	5-Hydroxytryptamine	A	Human	cryo-EM	7SRS	-	3.3	R	Active	100	60	Beta	Beta-arrestin-1	-	85	-	Fab light chain Fab heavy chain Fab30 heavy chain Fab30 light chain	Lysergide	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL	10.1016/J.NEURON.2022.08.006	2022-09-21	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7T2G	-	2.5	R	Active	100	70	Gi/o	αi1	-	62	BRIL	-	CHEMBL58362	small-molecule	Agonist	-	-	Yes	No	Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G	10.1038/S41589-022-01208-Y	2022-12-07	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7T2H	-	3.2	D	Active	100	71	Gi/o	αi1	-	61	-	scFv16	LOFENTANIL	small-molecule	Agonist	-	-	Yes	No	Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G	10.1038/S41589-022-01208-Y	2022-12-07	Yes
CRFR2	CRF₂	Corticotropin-releasing factor	B1	Human	cryo-EM	7TRY	-	3.7	P	Active	100	79	Gq/11	α11	-	60	-	-	Urocortin	peptide	Agonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2, urocortin 3	peptide	No	No	Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE	10.1038/S41467-022-33851-3	2022-11-09	Yes
CRFR2	CRF₂	Corticotropin-releasing factor	B1	Human	cryo-EM	7TS0	7TS0_refined	2.8	P	Active	100	72	Gi/o	αo	-	63	-	scFv16	Urocortin	peptide	Agonist	corticotrophin-releasing hormone, urocortin 1, urocortin 2, urocortin 3	peptide	No	No	Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE	10.1038/S41467-022-33851-3	2022-11-09	Yes
OPRM	μ	Opioid	A	Mouse	cryo-EM	7U2K	7U2K_refined	3.3	D	Active	100	71	Gi/o	αi1	-	61	-	-	CHEMBL147044	small-molecule	Agonist	-	-	Yes	No	Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S	10.1038/S41586-022-05588-Y	2022-12-07	Yes
FPR1	FPR1	Formylpeptide	A	Human	cryo-EM	7VFX	7VFX_refined	2.8	R	Active	100	84	Gi/o	αi1	-	62	-	scFv16	Peptide agonist fMet-Ile-Phe-Leu	peptide	Agonist	fMet-Leu-Phe, annexin I, spinorphin, cathepsin G	peptide	Yes	No	Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD	10.1038/S41467-022-32822-Y	2022-09-21	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7VIE	7VIE_refined	2.9	F	Active	100	73	Gi/o	αi1	-	64	-	scFv16	sphingosine 1-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R	10.1073/PNAS.2117716119	2022-09-28	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7VIF	-	2.8	F	Active	100	73	Gi/o	αi1	-	64	-	scFv16	(S)-FTY720-phosphate	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R	10.1073/PNAS.2117716119	2022-09-28	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7VIG	-	2.9	F	Active	100	73	Gi/o	αi1	-	63	-	scFv16	icanbelimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R	10.1073/PNAS.2117716119	2022-09-28	Yes
S1PR1	S1P₁	Lysophospholipid (S1P)	A	Human	cryo-EM	7VIH	-	3.0	F	Active	100	73	Gi/o	αi1	-	64	-	scFv16	icanbelimod	small-molecule	Agonist	sphingosylphosphorylcholine, sphingosine 1-phosphate	small-molecule	Yes	No	Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R	10.1073/PNAS.2117716119	2022-09-28	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7W6P	7W6P_refined	3.5	R	Active	100	55	Gi/o	αo	-	58	-	scFv16	N-pyridin-4-ylisoquinolin-4-amine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P	10.1126/SCIENCE.ABN7065	2022-09-28	Yes
ADA2A	α_2A	Adrenoceptors	A	Human	cryo-EM	7W7E	7W7E_refined	3.4	R	Active	100	56	Gi/o	αo	-	59	-	scFv16	5-(3-Bicyclo[4.2.0]octa-1,3,5-trienyl)-1,2,3,6-tetrahydropyridine	small-molecule	Agonist	(-)-adrenaline, (-)-noradrenaline	small-molecule	Yes	No	Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P	10.1126/SCIENCE.ABN7065	2022-09-28	Yes
GP119	GPR119	GPR18, GPR55 and GPR119	A	Human	cryo-EM	7WCM	7WCM_refined	2.3	R	Active	100	86	Gs	αs	-	60	-	Nanobody-35	MBX-2982	small-molecule	Agonist	anandamide, N-oleoylethanolamide, SEA, N-palmitoylethanolamine	small-molecule	Yes	No	Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A	10.1038/S41467-022-34696-6	2022-12-21	Yes
GP119	GPR119	GPR18, GPR55 and GPR119	A	Human	cryo-EM	7WCN	7WCN_refined	2.9	R	Active	100	86	Gs	αs	-	60	-	Nanobody-35	AR231453	small-molecule	Agonist	anandamide, N-oleoylethanolamide, SEA, N-palmitoylethanolamine	small-molecule	Yes	No	Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A	10.1038/S41467-022-34696-6	2022-12-21	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WXU	-	2.9	R	Active	100	30	Gq/11	αq	-	60	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y	10.1038/S41467-022-33173-4	2022-09-28	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WXW	-	2.8	R	Active	100	30	Gs	αs	Mini-Gs	56	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y	10.1038/S41467-022-33173-4	2022-09-28	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WY0	-	2.8	R	Active	100	30	G12/13	α13	-	55	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y	10.1038/S41467-022-33173-4	2022-09-28	Yes
AGRL3	ADGRL3	ADGRL	B2	Mouse	cryo-EM	7WY5	-	2.8	R	Active	100	17	Gq/11	αq	Mini-Gq	59	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y	10.1016/J.MOLCEL.2022.10.009	2022-10-26	Yes
AGRL3	ADGRL3	ADGRL	B2	Mouse	cryo-EM	7WY8	-	2.8	R	Active	100	17	Gs	αs	Mini-Gs	55	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y	10.1016/J.MOLCEL.2022.10.009	2022-10-26	Yes
AGRL3	ADGRL3	ADGRL	B2	Mouse	cryo-EM	7WYB	7WYB_refined	3.0	R	Active	100	17	Gi/o	αi1	-	64	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y	10.1016/J.MOLCEL.2022.10.009	2022-10-26	Yes
GPR88	GPR88	A orphans	A	Human	cryo-EM	7WZ4	7WZ4_refined	3.0	R	Active	100	61	Gi/o	αi1	-	61	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	Yes	No	Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y	10.1038/S41467-022-30081-5	2022-10-26	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7WZ7	-	2.8	R	Active	100	30	G12/13	α12	Mini-G12	52	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y	10.1038/S41467-022-33173-4	2022-09-28	Yes
AGRL3	ADGRL3	ADGRL	B2	Mouse	cryo-EM	7X10	-	2.9	R	Active	100	17	G12/13	α12	-	52	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y	10.1016/J.MOLCEL.2022.10.009	2022-11-09	Yes
AGRF1	ADGRF1	ADGRF	B2	Human	cryo-EM	7X2V	7X2V_refined	3.1	R	Active	100	30	Gi/o	αi1	-	62	-	scFv16	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y	10.1038/S41467-022-33173-4	2022-09-28	Yes
T2R46	TAS2R46	Taste 2	T	Human	cryo-EM	7XP4	-	3.0	R	Active	-	97	Gi/o	αt3	-	42	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T	10.1126/SCIENCE.ABO1633	2022-10-12	Yes
5HT5A	5-HT_5A	5-Hydroxytryptamine	A	Human	cryo-EM	7X5H	7X5H_refined	3.1	R	Active	100	77	Gi/o	αi1	-	63	BRIL	scFv16	5-CT	small-molecule	Agonist	5-hydroxytryptamine	small-molecule	Yes	No	Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y	10.1038/S41421-022-00412-3	2022-09-14	Yes
T2R46	TAS2R46	Taste 2	T	Human	cryo-EM	7XP5	-	3.1	R	Active	-	97	Gi/o	αt3	-	42	-	Nanobody-35	Apo (no ligand)	none	Apo (no ligand)	-	-	No	No	Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T	10.1126/SCIENCE.ABO1633	2022-10-12	Yes
T2R46	TAS2R46	Taste 2	T	Human	cryo-EM	7XP6	-	3.0	R	Active	-	92	Gi/o	αt3	-	42	-	Nanobody-35	strychnine	small-molecule	Agonist	-	-	No	No	Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T	10.1126/SCIENCE.ABO1633	2022-10-12	Yes
OX2R	OX₂	Orexin	A	Human	X-ray	7XRR	7XRR_refined	2.9	A	Inactive	1	70	-	-	-	-	-	-	lemborexant	small-molecule	Antagonist	orexin-A, orexin-B	peptide	No	No	Asada H, Im D, Hotta Y, Yasuda S, Murata T, Suno R, Iwata S	10.1016/J.STR.2022.11.001	2022-11-23	Yes
TRFR	TRH₁	Thyrotropin-releasing hormone	A	Human	cryo-EM	7XW9	7XW9_refined	2.7	R	Active	100	72	Gq/11	αq	-	63	-	scFv16	TRH	peptide	Agonist	TRH	peptide	Yes	No	-	-	2022-12-28	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7Y24	7Y24_refined	3.3	E	Active	100	77	Gi/o	αo	-	60	-	scFv16	Octreotide	peptide	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Chen S, Teng X, Zheng S	10.1038/S41589-022-01130-3	2022-10-19	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7Y26	-	3.3	E	Active	100	73	Gq/11	αq	Mini-Gq	62	-	scFv16	Octreotide	peptide	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Chen S, Teng X, Zheng S	10.1038/S41589-022-01130-3	2022-10-19	Yes
SSR2	SST2	Somatostatin	A	Human	cryo-EM	7Y27	-	3.5	E	Active	100	74	Gq/11	αq	Mini-Gq	64	-	scFv16	SOMATOSTATIN	protein	Agonist	CST-17, cortistatin-14, SRIF-28, SRIF-14	peptide	Yes	No	Chen S, Teng X, Zheng S	10.1038/S41589-022-01130-3	2022-10-19	Yes
GPR17	GPR17	A orphans	A	Human	cryo-EM	7Y89	7Y89_refined	3.0	A	Active	100	78	Gi/o	αi1	-	58	-	-	Apo (no ligand)	none	Apo (no ligand)	LTD₄, LTE₄, uridine diphosphate, ATP, LTC₄, UDP-glucose, UDP-galactose	small-molecule	Yes	No	Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y	10.1002/MCO2.159	2022-10-12	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU3	7YU3_refined	3.4	R	Active	100	80	Gi/o	αi1	-	63	-	scFv16	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU4	7YU4_refined	3.3	A	Active	99	73	-	-	-	-	-	-	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU5	7YU5_refined	3.3	R	Active	100	80	Gi/o	αi1	-	63	-	scFv16	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU6	7YU6_refined	3.5	R	Active	100	80	Gi/o	αi1	-	63	-	scFv16	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU7	7YU7_refined	3.8	R	Active	100	80	Gi/o	αi1	-	63	-	scFv16	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
LPAR1	LPA₁	Lysophospholipid (LPA)	A	Human	cryo-EM	7YU8	7YU8_refined	4.5	R	Active	100	80	Gi/o	αi1	-	63	-	scFv16	[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate	small-molecule	Agonist	1-O-Oleoyl-D-glycerol 3-phosphoric acid	small-molecule	Yes	No	Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O	10.1038/S41467-022-33121-2	2022-10-05	Yes
MRGX1	MRGPRX1	A orphans	A	Human	cryo-EM	8DWC	-	2.9	R	Active	100	78	Gs	αs	Gs-mini-Gq chimera	56	-	scFv16	Proenkephalin-A	peptide	Agonist	bovine adrenal medulla peptide 8-22	peptide	No	No	Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL	10.1038/S41589-022-01173-6	2022-11-02	Yes
MRGX1	MRGPRX1	A orphans	A	Human	cryo-EM	8DWG	-	2.7	R	Active	100	77	Gs	αs	Gs-mini-Gq chimera	56	-	scFv16	Proenkephalin-A 2-(Cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide	peptide small-molecule	Agonist PAM	bovine adrenal medulla peptide 8-22	peptide	No	No	Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL	10.1038/S41589-022-01173-6	2022-11-02	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	8HAF	-	3.3	R	Active	100	62	Gs	αs	-	56	-	Nanobody-35	PTHrP-(1-36)	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE	10.1038/S41401-022-01032-Z	2022-12-21	Yes
MRGX1	MRGPRX1	A orphans	A	Human	cryo-EM	8DWH	-	3.3	R	Active	100	77	Gs	αs	Gs-mini-Gq chimera	56	-	-	compound 16 [PMID: 31498617]	small-molecule	Agonist	bovine adrenal medulla peptide 8-22	peptide	No	No	Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL	10.1038/S41589-022-01173-6	2022-11-02	Yes
OPRX	NOP	Opioid	A	Human	cryo-EM	8F7X	8F7X_refined	3.3	R	Active	100	77	Gi/o	αi1	-	62	-	scFv16	nociceptin/orphanin FQ	peptide	Agonist	nociceptin/orphanin FQ	peptide	Yes	No	Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE	10.1016/J.CELL.2022.12.026	2022-12-14	Yes
PACR	PAC₁	VIP and PACAP	B1	Human	cryo-EM	8E3X	8E3X_refined	2.3	R	Active	100	77	Gs	αs	-	59	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, PHI, PACAP-38, VIP, PHV	peptide	No	No	Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D	10.1038/S41467-022-34629-3	2022-11-23	Yes
VIPR1	VPAC₁	VIP and PACAP	B1	Human	cryo-EM	8E3Y	-	2.3	R	Active	100	81	Gs	αs	-	56	-	Nanobody-35	[Ac-His¹]PACAP-27	peptide	Agonist	PACAP-27, PHM, secretin, GHRH, PACAP-38, VIP, PHI	peptide	No	No	Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D	10.1038/S41467-022-34629-3	2022-11-23	Yes
VIPR1	VPAC₁	VIP and PACAP	B1	Human	cryo-EM	8E3Z	8E3Z_refined	2.7	R	Active	100	81	Gs	αs	-	55	-	Nanobody-35	Vasoactive intestinal polypeptide	small-molecule	Agonist	PACAP-27, PHM, secretin, GHRH, PACAP-38, VIP, PHI	peptide	No	No	Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D	10.1038/S41467-022-34629-3	2022-11-23	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Human	cryo-EM	8E9W	-	2.7	A	Active	100	47	Gq/11	αq	mini-Gq	59	-	scFv16	CHEMBL73538	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL	10.1038/S41586-022-05489-0	2022-11-30	Yes
ACM4	M₄	Acetylcholine (muscarinic)	A	Human	cryo-EM	8E9X	-	2.7	A	Active	100	57	Gi/o	αo	mini-Go	58	-	scFv16	CHEMBL73538	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL	10.1038/S41586-022-05489-0	2022-11-30	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Human	cryo-EM	8E9Y	-	2.8	A	Active	100	47	Gq/11	αq	mini-Gq	61	-	scFv16	Clozapine N-oxide	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL	10.1038/S41586-022-05489-0	2022-11-30	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Human	cryo-EM	8E9Z	-	2.7	A	Active	100	47	Gq/11	αq	mini-Gq	62	-	scFv16	iperoxo	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL	10.1038/S41586-022-05489-0	2022-11-30	Yes
ACM3	M₃	Acetylcholine (muscarinic)	A	Human	cryo-EM	8EA0	8EA0_refined	2.6	A	Active	99	48	-	-	-	-	-	-	iperoxo	small-molecule	Agonist	acetylcholine	small-molecule	Yes	No	Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL	10.1038/S41586-022-05489-0	2022-11-30	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EF5	-	3.3	R	Active	100	72	Gi/o	αi1	-	64	-	scFv16	fentanyl	small-molecule	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EF6	8EF6_refined	3.2	R	Active	100	72	Gi/o	αi1	-	64	-	scFv16	morphine	small-molecule	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EFB	8EFB_refined	3.2	R	Active	100	71	Gi/o	αi1	-	64	-	scFv16	OLICERIDINE	small-molecule	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EFL	8EFL_refined	3.2	R	Active	100	72	Gi/o	αi1	-	64	-	scFv16	CHEMBL4452384	small-molecule	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EFO	8EFO_refined	2.8	R	Active	100	72	Gi/o	αi1	-	64	-	scFv16	PZM21	small-molecule	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8EFQ	-	3.3	R	Active	100	71	Gi/o	αi1	-	61	-	-	DAMGO	peptide	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE	10.1016/J.CELL.2022.09.041	2022-11-09	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8F7Q	-	3.2	R	Active	100	72	Gi/o	αi1	-	64	-	scFv16	β-endorphin	peptide	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE	10.1016/J.CELL.2022.12.026	2022-12-14	Yes
OPRM	μ	Opioid	A	Human	cryo-EM	8F7R	8F7R_refined	3.3	R	Active	100	72	Gi/o	αi1	-	63	-	scFv16	endomorphin-1	peptide	Agonist	endomorphin-1, endomorphin-2, dynorphin A, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE	10.1016/J.CELL.2022.12.026	2022-12-14	Yes
OPRD	δ	Opioid	A	Human	cryo-EM	8F7S	8F7S_refined	3.0	R	Active	100	78	Gi/o	αi1	-	62	-	-	DELTORPHIN II	protein	Agonist	endomorphin-1, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	No	No	Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE	10.1016/J.CELL.2022.12.026	2022-12-14	Yes
OPRK	κ	Opioid	A	Human	cryo-EM	8F7W	8F7W_refined	3.2	R	Active	100	75	Gi/o	αi1	-	64	-	scFv16	dynorphin A-(1-8)	peptide	Agonist	big dynorphin, β-neoendorphin, dynorphin A, α-neoendorphin, [Leu]enkephalin, dynorphin A-(1-13), dynorphin A-(1-8), [Met]enkephalin, dynorphin B, β-endorphin	peptide	Yes	No	Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE	10.1016/J.CELL.2022.12.026	2022-12-14	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	8HA0	-	2.6	R	Active	100	61	Gs	αs	-	56	-	Nanobody-35	teriparatide	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE	10.1038/S41401-022-01032-Z	2022-12-21	Yes
PTH1R	PTH1	Parathyroid hormone	B1	Human	cryo-EM	8HAO	-	3.8	R	Active	100	61	Gs	αs	-	56	-	Nanobody-35	teriparatide	peptide	Agonist	TIP39, PTHrP, PTH, PTHrP-(1-36)	peptide	No	No	Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE	10.1038/S41401-022-01032-Z	2022-12-21	Yes